Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 38, Issue 1 (2023)

Browse this journal
Sample our Medicine, Dentistry, Nursing & Allied Health journals, sign in here to start your FREE access for 14 days

Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 38, Issue 1 (2023)

See all volumes and issues
Vol 39, 2024 Volume 38, 2023 Vol 37, 2022 Vol 36, 2021 Vol 35, 2020 Vol 34, 2019 Vol 33, 2018 Vol 32, 2017 Vol 31, 2016 Vol 30, 2015 Vol 29, 2014 Vol 28, 2013 Vol 27, 2012 Vol 26, 2011 Vol 25, 2010 Vol 24, 2009 Vol 23, 2008 Vol 22, 2007 Vol 21, 2006 Vol 20, 2005 Vol 19, 2004 Vol 18, 2003 Vol 17, 2002 Vol 16, 2001 Vol 15, 1999-2000 Vol 14, 1998-1999 Vol 13, 1998 Vol 12, 1997 Vol 11, 1996-1997 Vol 10, 1995-1996 Vol 9, 1995 Vol 8, 1994-1995 Vol 7, 1993 Vol 6, 1992-1993 Vol 5, 1991 Vol 4, 1990-1991 Vol 3, 1989-1990 Vol 2, 1987-1989 Vol 1, 1985-1987
Download citations Download PDFs

Research Paper

Article
Combining nano-differential scanning fluorimetry and microscale thermophoresis to investigate VDAC1 interaction with small molecules
Hubert Gorny, Angélique Mularoni, Jean-Guy Delcros, Céline Freton, Jordane Preto & Isabelle Krimm
Article: 2121821
Published online: 17 Jan 2023
AbstractforCombining nano-differential scanning fluorimetry and microscale thermophoresis to investigate VDAC1 interaction with small molecules | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1740 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities
Mostafa M. M. El-Miligy, Marwa E. Abdelaziz, Salwa M. Fahmy, Tamer M. Ibrahim, Marwa M. Abu-Serie, Mona A. Mahran & Aly A. Hazzaa
Article: 2152810
Published online: 11 Jan 2023
AbstractforDiscovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities | Full Text | References | PDF (5.5 MB) | EPUB | Supplemental
  • 1960 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors
Morteza Abdoli, Alessandro Bonardi, Claudiu T. Supuran & Raivis Žalubovskis
Article: 2152811
Published online: 11 Jan 2023
AbstractforInvestigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors | Full Text | References | PDF (1.9 MB) | EPUB
  • 1189 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Identification of a new structural family of SGK1 inhibitors as potential neuroprotective agents
Ines Maestro, Enrique Madruga, Patricia Boya & Ana Martínez
Article: 2153841
Published online: 13 Jan 2023
AbstractforIdentification of a new structural family of SGK1 inhibitors as potential neuroprotective agents | Full Text | References | PDF (3.2 MB) | EPUB
  • 1530 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of new 6-ureido/amidocoumarins as highly potent and selective inhibitors for the tumour-relevant carbonic anhydrases IX and XII
Ashraf K. El-Damasy, Hyun Ji Kim, Alessio Nocentini, Seon Hee Seo, Wagdy M. Eldehna, Eun-Kyoung Bang, Claudiu T. Supuran & Gyochang Keum
Article: 2154603
Published online: 02 Feb 2023
AbstractforDiscovery of new 6-ureido/amidocoumarins as highly potent and selective inhibitors for the tumour-relevant carbonic anhydrases IX and XII | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 1563 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and evaluation of 2, 6, 8-substituted Imidazopyridine derivatives as potent PI3Kα inhibitors
Rui Chen, Zhongyuan Wang, Lijie Sima, Hu Cheng, Bilan Luo, Jianta Wang, Bing Guo, Shunyi Mao, Zhixu Zhou, Jingang Peng, Lei Tang, Xinfu Liu & Weike Liao
Article: 2155638
Published online: 17 Jan 2023
AbstractforDesign, synthesis and evaluation of 2, 6, 8-substituted Imidazopyridine derivatives as potent PI3Kα inhibitors | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 1588 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review
Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium: a comprehensive review
Lin Wang, Siyu Chen, Xun Gao, Xiao Liang, Weichen Lv, Dongfang Zhang & Xin Jin
Article: 2155639
Published online: 11 Jan 2023
AbstractforRecent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium: a comprehensive review | Full Text | References | PDF (9.9 MB) | EPUB
  • 2482 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P-glycoprotein expression levels
Laila M. Al-Harbi, Eman A. Al-Harbi, Rawda M. Okasha, R. A. El-Eisawy, Mohammed A. A. El-Nassag, Hany M. Mohamed, Ahmed M. Fouda, Ahmed A. Elhenawy, Ahmed Mora, Ahmed M. El-Agrody & Heba K. A. El-Mawgoud
Article: 2155814
Published online: 20 Jan 2023
AbstractforDiscovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P-glycoprotein expression levels | Full Text | References | PDF (4.3 MB) | EPUB | Supplemental
  • 1448 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation
Wei Liu, Youyou He, Zhongjie Guo, Miaomiao Wang, Xiaodong Han, Hairui Jia, Jin He, Shanshan Miao & Shengzheng Wang
Article: 2155815
Published online: 11 Jan 2023
AbstractforDiscovery of potent tubulin inhibitors targeting the colchicine binding site via structure-based lead optimization and antitumor evaluation | Full Text | References | PDF (5.4 MB) | EPUB | Supplemental
  • 2039 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review
Selected strategies to fight pathogenic bacteria
Aiva Plotniece, Arkadij Sobolev, Claudiu T. Supuran, Fabrizio Carta, Fredrik Björkling, Henrik Franzyk, Jari Yli-Kauhaluoma, Koen Augustyns, Paul Cos, Linda De Vooght, Matthias Govaerts, Juliana Aizawa, Päivi Tammela & Raivis Žalubovskis
Article: 2155816
Published online: 11 Jan 2023
AbstractforSelected strategies to fight pathogenic bacteria | Full Text | References | PDF (3.7 MB) | EPUB
  • 3727 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Discovery of novel enasidenib analogues targeting inhibition of mutant isocitrate dehydrogenase 2 as antileukaemic agents
Ahmed F. Khalil, Tarek F. El-Moselhy, Eman A. El-Bastawissy, Rasha Abdelhady, Nancy S. Younis & Mervat H. El-Hamamsy
Article: 2157411
Published online: 11 Jan 2023
AbstractforDiscovery of novel enasidenib analogues targeting inhibition of mutant isocitrate dehydrogenase 2 as antileukaemic agents | Full Text | References | PDF (5 MB) | EPUB | Supplemental
  • 1354 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Design and synthesis of novel rigid dibenzo[b,f]azepines through ring closure technique as promising anticancer candidates against leukaemia and acting as selective topoisomerase II inhibitors and DNA intercalators
Mohammed Farrag El-Behairy, Walaa Hamada Abd-Allah, Mohamed M. Khalifa, Mohamed S. Nafie, Mohamed A. Saleh, Mohammed S. Abdel-Maksoud, Tarfah Al-Warhi, Wagdy M. Eldehna & Ahmed A. Al‐Karmalawy
Article: 2157825
Published online: 11 Jan 2023
AbstractforDesign and synthesis of novel rigid dibenzo[b,f]azepines through ring closure technique as promising anticancer candidates against leukaemia and acting as selective topoisomerase II inhibitors and DNA intercalators | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
  • 1708 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Aromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors
D. Zelencova-Gopejenko, V. Andrianov, I. Domracheva, I. Kanepe-Lapsa, M. Milczarek, M. Stojak, K. Przyborowski, F. A. Fedak, M. Walczak, K. Kramkowski, J. Wietrzyk, S. Chlopicki & I. Kalvins
Article: 2158187
Published online: 18 Apr 2023
AbstractforAromatic sulphonamides of aziridine-2-carboxylic acid derivatives as novel PDIA1 and PDIA3 inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1373 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
New cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer’s disease
Kamila Czarnecka, Małgorzata Girek, Paweł Kręcisz, Robert Skibiński, Kamil Łątka, Jakub Jończyk, Marek Bajda, Piotr Szymczyk, Grzegorz Galita, Jacek Kabziński, Ireneusz Majsterek, Alba Espargaró, Raimon Sabate & Paweł Szymański
Article: 2158822
Published online: 11 Jan 2023
AbstractforNew cyclopentaquinoline and 3,5-dichlorobenzoic acid hybrids with neuroprotection against oxidative stress for the treatment of Alzheimer’s disease | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 2381 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of novel 2-(4-(benzyloxy)-5-(hydroxyl) phenyl) benzothiazole derivatives as multifunctional MAO-B inhibitors for the treatment of Parkinson’s disease
Zhongcheng Cao, Xingyue Wang, Tianlong Zhang, Xianwu Fu, Fan Zhang & Jiang Zhu
Article: 2159957
Published online: 02 Feb 2023
AbstractforDiscovery of novel 2-(4-(benzyloxy)-5-(hydroxyl) phenyl) benzothiazole derivatives as multifunctional MAO-B inhibitors for the treatment of Parkinson’s disease | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1786 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
An in silico toolbox for the prediction of the potential pathogenic effects of missense mutations in the dimeric region of hRPE65
Giulio Poli, Gian Carlo Demontis, Andrea Sodi, Alessandro Saba, Stanislao Rizzo, Marco Macchia & Tiziano Tuccinardi
Article: 2162047
Published online: 11 Jan 2023
AbstractforAn in silico toolbox for the prediction of the potential pathogenic effects of missense mutations in the dimeric region of hRPE65 | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1007 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents
Mohammad M. Al-Sanea, Abdelrahman Hamdi, Simone Brogi, Samar S. Tawfik, Dina I. A. Othman, Mahmoud Elshal, Hidayat Ur Rahman, Della G. T. Parambi, Rehab M. Elbargisy, Samy Selim, Ehab M. Mostafa & Ahmed A. B. Mohamed
Article: 2162511
Published online: 12 Jan 2023
AbstractforDesign, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents | Full Text | References | PDF (4 MB) | EPUB | Supplemental
  • 1623 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents
Yu-Shun Yang, Bin Wang, Junzhong Liu, Qin Li, Qin-Cai Jiao & Pei Qin
Article: 2163241
Published online: 11 Jan 2023
AbstractforDiscovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1082 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells
Aide Negri, Marina Marozzi, Daniela Trisciuoglio, Dante Rotili, Antonello Mai & Federica Rizzi
Article: 2163242
Published online: 11 Jan 2023
AbstractforSimultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 2179 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel thiazolone-benzenesulphonamide inhibitors of human and bacterial carbonic anhydrases
Morteza Abdoli, Viviana De Luca, Clemente Capasso, Claudiu T. Supuran & Raivis Žalubovskis
Article: 2163243
Published online: 11 Jan 2023
AbstractforNovel thiazolone-benzenesulphonamide inhibitors of human and bacterial carbonic anhydrases | Full Text | References | PDF (1.9 MB) | EPUB
  • 1180 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells
Guanglong Zhang, Zhenhua Tang, Sili Fan, Chengpeng Li, Yan Li, Weiqin Liu, Xuesha Long, Wenjing Zhang, Yi Zhang, Zhurui Li, Zhenchao Wang, Danping Chen & Guiping Ouyang
Article: 2163393
Published online: 11 Jan 2023
AbstractforSynthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
  • 2022 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, kinetic studies and in-silico investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors
Muhammad Naeem Mustafa, Pervaiz Ali Channar, Muhammad Sarfraz, Aamer Saeed, Syeda Abida Ejaz, Mubashir Aziz, Fatmah Ali Alasmary, Hanadi Yaqob Alsoqair, Hussain Raza, Song Ja Kim & Asad Hamad
Article: 2163394
Published online: 11 Jan 2023
AbstractforSynthesis, kinetic studies and in-silico investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1725 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, molecular modelling and antitumor evaluation of S-glucosylated rhodanines through topo II inhibition and DNA intercalation
Ahmed I. Khodair, Fatimah M. Alzahrani, Mohamed K. Awad, Siham A. Al-Issa, Ghaferah H. Al-Hazmi & Mohamed S. Nafie
Article: 2163996
Published online: 11 Jan 2023
AbstractforDesign, synthesis, molecular modelling and antitumor evaluation of S-glucosylated rhodanines through topo II inhibition and DNA intercalation | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
  • 1306 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
New isoxazolidinyl-based N-alkylethanolamines as new activators of human brain carbonic anhydrases
Doretta Cuffaro, Riccardo Di Leo, Lidia Ciccone, Alessio Nocentini, Claudiu T. Supuran, Elisa Nuti & Armando Rossello
Article: 2164574
Published online: 11 Jan 2023
AbstractforNew isoxazolidinyl-based N-alkylethanolamines as new activators of human brain carbonic anhydrases | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1051 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Synthesis and structure–activity relationships of pyrazole-based inhibitors of meprin α and β
Kathrin Tan, Christian Jäger, Stefanie Geissler, Dagmar Schlenzig, Mirko Buchholz & Daniel Ramsbeck
Article: 2165648
Published online: 20 Jan 2023
AbstractforSynthesis and structure–activity relationships of pyrazole-based inhibitors of meprin α and β | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1126 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Review

Review
ALDEFLUOR activity, ALDH isoforms, and their clinical significance in cancers
Jiang-Jie Duan, Jiao Cai, Lei Gao & Shi-Cang Yu
Article: 2166035
Published online: 18 Jan 2023
AbstractforALDEFLUOR activity, ALDH isoforms, and their clinical significance in cancers | Full Text | References | PDF (2.4 MB) | EPUB
  • 1952 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study
Mohammad M. Al-Sanea, Abdelrahman Hamdi, Ahmed A. B. Mohamed, Hamed W. El-Shafey, Mahmoud Moustafa, Abdullah A. Elgazar, Wagdy M. Eldehna, Hidayat Ur Rahman, Della G. T. Parambi, Rehab M. Elbargisy, Samy Selim, Syed Nasir Abbas Bukhari, Omnia Magdy Hendawy & Samar S. Tawfik
Article: 2166036
Published online: 24 Jan 2023
AbstractforNew benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 2897 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Article
Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico studies
Dina I. A. Othman, Abdelrahman Hamdi, Samar S. Tawfik, Abdullah A. Elgazar & Amany S. Mostafa
Article: 2166037
Published online: 18 Jan 2023
AbstractforIdentification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico studies | Full Text | References | PDF (3.9 MB) | EPUB | Supplemental
  • 2867 Views
  • 21 CrossRef citations
  • 0Altmetric
Open Access
Article
In silico identification and biological evaluation of a selective MAP4K4 inhibitor against pancreatic cancer
Chao-Di Chang, Min-Wu Chao, Hsueh-Yun Lee, Yi-Ting Liu, Huang-Ju Tu, Ssu-Ting Lien, Tony Eight Lin, Tzu-Ying Sung, Shih-Chung Yen, Sing-Han Huang, Kai-Cheng Hsu & Shiow-Lin Pan
Article: 2166039
Published online: 22 Jan 2023
AbstractforIn silico identification and biological evaluation of a selective MAP4K4 inhibitor against pancreatic cancer | Full Text | References | PDF (4.4 MB) | EPUB | Supplemental
  • 2287 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Dual-target ligand discovery for Alzheimer’s disease: triphenylphosphoranylidene derivatives as inhibitors of acetylcholinesterase and β-amyloid aggregation
Marwa El-Hussieny, Mansoura A. Abd-El-Maksoud, Fouad M. Soliman, Marwa A. Fouad & Mohamed K. El-Ashrey
Article: 2166040
Published online: 24 Jan 2023
AbstractforDual-target ligand discovery for Alzheimer’s disease: triphenylphosphoranylidene derivatives as inhibitors of acetylcholinesterase and β-amyloid aggregation | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 2172 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Review

Review
Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications
Andrea Angeli & Claudiu T. Supuran
Article: 2166503
Published online: 13 Jan 2023
AbstractforClick chemistry approaches for developing carbonic anhydrase inhibitors and their applications | Full Text | References | PDF (4.2 MB) | EPUB
  • 2301 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Design, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study
Mohammad M. Al-Sanea, Tamer M. Nasr, Samir Bondock, Aya Y. Gawish & Nada M. Mohamed
Article: 2166936
Published online: 02 Feb 2023
AbstractforDesign, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study | Full Text | References | PDF (7.3 MB) | EPUB | Supplemental
  • 1437 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
TXNIP inhibition in the treatment of type 2 diabetes mellitus: design, synthesis, and biological evaluation of quinazoline derivatives
Aiyun Li, Li Guan, Wanzhen Su, Ning Zhao, Xuwen Song, Jin Wang, Xiaoxiao Tang, Weize Li & Xiangying Jiao
Article: 2166937
Published online: 18 Jan 2023
AbstractforTXNIP inhibition in the treatment of type 2 diabetes mellitus: design, synthesis, and biological evaluation of quinazoline derivatives | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1737 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Purification and characterisation of glutathione reductase from scorpionfish (scorpaena porcus) and investigation of heavy metal ions inhibition
Kübra Işık & Ercan Soydan
Article: 2167078
Published online: 20 Mar 2023
AbstractforPurification and characterisation of glutathione reductase from scorpionfish (scorpaena porcus) and investigation of heavy metal ions inhibition | Full Text | References | PDF (572.2 KB) | EPUB | Supplemental
  • 1046 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
Sulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasite Gyrodactylus salaris
Ashok Aspatwar, Alessandro Bonardi, Heidi Aisala, Ksenia Zueva, Craig R Primmer, Jaakko Lumme, Seppo Parkkila & Claudiu T. Supuran
Article: 2167988
Published online: 17 Jan 2023
AbstractforSulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasite Gyrodactylus salaris | Full Text | References | PDF (1.1 MB) | EPUB
  • 1018 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Design, synthesis and biological evaluation of 2-((4-sulfamoylphenyl)amino)-pyrrolo[2,3-d]pyrimidine derivatives as CDK inhibitors
Bo Yang, Yanni Quan, Wuli Zhao, Yingjie Ji, Xiaotang Yang, Jianrui Li, Yi Li, Xiujun Liu, Ying Wang & Yanping Li
Article: 2169282
Published online: 19 Jan 2023
AbstractforDesign, synthesis and biological evaluation of 2-((4-sulfamoylphenyl)amino)-pyrrolo[2,3-d]pyrimidine derivatives as CDK inhibitors | Full Text | References | PDF (4.5 MB) | EPUB
  • 1932 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and evaluation of quinoline-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease
Hongsong Chen, Jing Mi, Sen Li, Zhengwei Liu, Jing Yang, Rui Chen, Yujie Wang, Yujuan Ban, Yi Zhou, Wu Dong & Zhipei Sang
Article: 2169682
Published online: 23 Jan 2023
AbstractforDesign, synthesis and evaluation of quinoline-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease | Full Text | References | PDF (5 MB) | EPUB | Supplemental
  • 3047 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
The importance of including the C-terminal domain of PTP1B1-400 to identify potential antidiabetic inhibitors
Andrea Coronell-Tovar, Francisco Cortés-Benítez & Martin González-Andrade
Article: 2170369
Published online: 30 Mar 2023
AbstractforThe importance of including the C-terminal domain of PTP1B1-400 to identify potential antidiabetic inhibitors | Full Text | References | PDF (2.7 MB) | EPUB
  • 1298 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Derivatives of 4-methyl-1,2,3-benzoxathiazine 2,2-dioxide as selective inhibitors of human carbonic anhydrases IX and XII over the cytosolic isoforms I and II
Jekaterīna Ivanova, Morteza Abdoli, Alessio Nocentini, Raivis Žalubovskis & Claudiu T. Supuran
Article: 2170370
Published online: 31 Jan 2023
AbstractforDerivatives of 4-methyl-1,2,3-benzoxathiazine 2,2-dioxide as selective inhibitors of human carbonic anhydrases IX and XII over the cytosolic isoforms I and II | Full Text | References | PDF (2.7 MB) | EPUB
  • 887 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access

Review

Review
Research progress of natural products and their derivatives against Alzheimer’s disease
Jin-Ying Liu, Hong-Yan Guo, Zhe-Shan Quan, Qing-Kun Shen, Hong Cui & Xiaoting Li
Article: 2171026
Published online: 20 Feb 2023
AbstractforResearch progress of natural products and their derivatives against Alzheimer’s disease | Full Text | References | PDF (2 MB) | EPUB
  • 3890 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Carboranyl-1,8-naphthalimide intercalators induce lysosomal membrane permeabilization and ferroptosis in cancer cell lines
Sebastian Rykowski, Dorota Gurda-Woźna, Agnieszka Fedoruk-Wyszomirska, Marta Orlicka-Płocka, Aleksandra Kowalczyk, Paweł Stączek, Marta Denel-Bobrowska, Katarzyna Biniek-Antosiak, Wojciech Rypniewski, Eliza Wyszko & Agnieszka B. Olejniczak
Article: 2171028
Published online: 30 Jan 2023
AbstractforCarboranyl-1,8-naphthalimide intercalators induce lysosomal membrane permeabilization and ferroptosis in cancer cell lines | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
  • 2177 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro, molecular docking, molecular dynamics, and SAR studies
Faten Farouk, Ayman Abo Elmaaty, Ahmed Elkamhawy, Haytham O. Tawfik, Radwan Alnajjar, Mohammed A. S. Abourehab, Mohamed A. Saleh, Wagdy M. Eldehna & Ahmed A. Al‐Karmalawy
Article: 2171029
Published online: 26 Jan 2023
AbstractforInvestigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro, molecular docking, molecular dynamics, and SAR studies | Full Text | References | PDF (5.4 MB) | EPUB | Supplemental
  • 2780 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Article
Adiponectin – stratification biomarker in diastolic cardiac dysfunction
Valeriu-Gabi Dincă, Adriana Diaconu, Bogdan-Ioan Coculescu, Alexandra-Ligia Dincă, Diana Mihaela Ciuc, Rodica Daniela Bîrlă, Cristian Daniel Marica, Sorin Ioan Tudorache, Gheorghe Manole & Elena Claudia Coculescu
Article: 2171030
Published online: 24 Jan 2023
AbstractforAdiponectin – stratification biomarker in diastolic cardiac dysfunction | Full Text | References | PDF (1.3 MB) | EPUB
  • 1310 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
Inhibition studies with simple and complex (in)organic anions of the γ-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri, MscCAγ
Simone Giovannuzzi, Viviana De Luca, Clemente Capasso & Claudiu T. Supuran
Article: 2173748
Published online: 31 Jan 2023
AbstractforInhibition studies with simple and complex (in)organic anions of the γ-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri, MscCAγ | Full Text | References | PDF (886.6 KB) | EPUB
  • 843 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
2-((1H-Benzo[d]imidazol-2-yl)amino)benzo[d]thiazole-6-sulphonamides: a class of carbonic anhydrase II and VII-selective inhibitors
Morteza Abdoli, Claudiu T. Supuran & Raivis Žalubovskis
Article: 2174981
Published online: 10 Feb 2023
Abstractfor2-((1H-Benzo[d]imidazol-2-yl)amino)benzo[d]thiazole-6-sulphonamides: a class of carbonic anhydrase II and VII-selective inhibitors | Full Text | References | PDF (2.5 MB) | EPUB
  • 1336 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2-a] pyrimidines as topoisomerase II inhibitors
Mona S. El-Zoghbi, Samiha A. El-Sebaey, Hanan A. AL-Ghulikah & Eman A. Sobh
Article: 2175209
Published online: 12 Feb 2023
AbstractforDesign, synthesis, docking, and anticancer evaluations of new thiazolo[3,2-a] pyrimidines as topoisomerase II inhibitors | Full Text | References | PDF (5.8 MB) | EPUB | Supplemental
  • 1729 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and biological evaluation of benzoheterocyclic sulfoxide derivatives as quorum sensing inhibitors in Pseudomonas aeruginosa
Shen Mao, Qiaoqiang Li, Zhikun Yang, Yasheng Li, Xinyi Ye & Hong Wang
Article: 2175820
Published online: 07 Feb 2023
AbstractforDesign, synthesis, and biological evaluation of benzoheterocyclic sulfoxide derivatives as quorum sensing inhibitors in Pseudomonas aeruginosa | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1675 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel benzothiazole derivatives as multitargeted-directed ligands for the treatment of Alzheimer’s disease
Donia E. Hafez, Mariam Dubiel, Gabriella La Spada, Marco Catto, David Reiner-Link, Yu-Ting Syu, Mohammad Abdel-Halim, Tsong-Long Hwang, Holger Stark & Ashraf H. Abadi
Article: 2175821
Published online: 15 Feb 2023
AbstractforNovel benzothiazole derivatives as multitargeted-directed ligands for the treatment of Alzheimer’s disease | Full Text | References | PDF (5.4 MB) | EPUB | Supplemental
  • 2662 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access

Correction

Correction
Correction
Article: 2177411
Published online: 08 Feb 2023
First Page PreviewforCorrection | Full Text | PDF (628.2 KB) | EPUB
  • 405 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Diversely N-substituted benzenesulfonamides dissimilarly bind to human carbonic anhydrases: crystallographic investigations of N-nitrosulfonamides
Andrea Angeli, Marta Ferraroni, Alessandro Bonardi, Claudiu T. Supuran & Alessio Nocentini
Article: 2178430
Published online: 16 Feb 2023
AbstractforDiversely N-substituted benzenesulfonamides dissimilarly bind to human carbonic anhydrases: crystallographic investigations of N-nitrosulfonamides | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 1045 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Different chemical proteomic approaches to identify the targets of lapatinib
Tatjana Kovačević, Krunoslav Nujić, Mario Cindrić, Snježana Dragojević, Adrijana Vinter, Amela Hozić & Milan Mesić
Article: 2183809
Published online: 01 Mar 2023
AbstractforDifferent chemical proteomic approaches to identify the targets of lapatinib | Full Text | References | PDF (1.6 MB) | EPUB
  • 1078 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Effect of in vitro simulated digestion on the anti-Helicobacter Pylori activity of different Propolis extracts
Paolo Governa, Giulia Romagnoli, Paola Albanese, Federico Rossi, Fabrizio Manetti & Marco Biagi
Article: 2183810
Published online: 14 Mar 2023
AbstractforEffect of in vitro simulated digestion on the anti-Helicobacter Pylori activity of different Propolis extracts | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1493 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Cloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke, Schistosoma mansoni
Susanna Haapanen, Andrea Angeli, Martti Tolvanen, Reza Zolfaghari Emameh, Claudiu T. Supuran & Seppo Parkkila
Article: 2184299
Published online: 01 Mar 2023
AbstractforCloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke, Schistosoma mansoni | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 985 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological evaluation of new 3-substituted coumarin derivatives as selective inhibitors of human carbonic anhydrase IX and XII
Shaik Mahammad Ghouse, Kavyaraj Bahatam, Andrea Angeli, Gaurav Pawar, Krishna Kartheek Chinchilli, Venkata Madhavi Yaddanapudi, Arifuddin Mohammed, Claudiu T. Supuran & Srinivas Nanduri
Article: 2185760
Published online: 06 Mar 2023
AbstractforSynthesis and biological evaluation of new 3-substituted coumarin derivatives as selective inhibitors of human carbonic anhydrase IX and XII | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1718 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
WRH-2412 alleviates the progression of hepatocellular carcinoma through regulation of TGF-β/β-catenin/α-SMA pathway
Mohammed A. F. Elewa, Wagdy M. Eldehna, Ahmed M. E. Hamdan, Samraa H. Abd El-kawi, Asmaa M. El-Kalaawy, Taghreed A. Majrashi, Reham F. Barghash, Hatem A. Abdel-Aziz, Khalid S. Hashem & Mohammed M. H. Al-Gayyar
Article: 2185761
Published online: 13 Mar 2023
AbstractforWRH-2412 alleviates the progression of hepatocellular carcinoma through regulation of TGF-β/β-catenin/α-SMA pathway | Full Text | References | PDF (2.7 MB) | EPUB
  • 1690 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Potent carbonic anhydrase I, II, IX and XII inhibition activity of novel primary benzenesulfonamides incorporating bis-ureido moieties
Tuba Tekeli, Suleyman Akocak, Andrea Petreni, Nebih Lolak, Servet Çete & Claudiu T. Supuran
Article: 2185762
Published online: 02 Mar 2023
AbstractforPotent carbonic anhydrase I, II, IX and XII inhibition activity of novel primary benzenesulfonamides incorporating bis-ureido moieties | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 1170 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, biological evaluation, and molecular modelling insights of cupressic acid derivatives as promising anti-inflammatory agents
Amal F. Soliman, Diaaeldin M. Elimam, Fardous F. El-Senduny, Manal A. Alossaimi, Mubarak Alamri & Fatma M. Abdel Bar
Article: 2187327
Published online: 13 Mar 2023
AbstractforDesign, biological evaluation, and molecular modelling insights of cupressic acid derivatives as promising anti-inflammatory agents | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 1092 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Antihistamines, phenothiazine-based antipsychotics, and tricyclic antidepressants potently activate pharmacologically relevant human carbonic anhydrase isoforms II and VII
Francesco Fiorentino, Alessio Nocentini, Dante Rotili, Claudiu T. Supuran & Antonello Mai
Article: 2188147
Published online: 13 Mar 2023
AbstractforAntihistamines, phenothiazine-based antipsychotics, and tricyclic antidepressants potently activate pharmacologically relevant human carbonic anhydrase isoforms II and VII | Full Text | References | PDF (1.8 MB) | EPUB
  • 1220 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Short Communication

Brief Report
Overcoming the imatinib-resistant BCR-ABL mutants with new ureidobenzothiazole chemotypes endowed with potent and broad-spectrum anticancer activity
Ashraf K. El-Damasy, Heewon Jin, Jung Woo Park, Hyun Ji Kim, Hanan Khojah, Seon Hee Seo, Ju-Hyeon Lee, Eun-Kyoung Bang & Gyochang Keum
Article: 2189097
Published online: 17 Mar 2023
AbstractforOvercoming the imatinib-resistant BCR-ABL mutants with new ureidobenzothiazole chemotypes endowed with potent and broad-spectrum anticancer activity | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1484 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Synthesis, biological evaluation and theoretical studies of (E)-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibitors
Farhat Ramzan, Syed Ayaz Nabi, Mehak Saba Lone, Alessandro Bonardi, Aabid Hamid, Sameena Bano, Kalicharan Sharma, Syed Shafi, Mohammed Samim, Kalim Javed & Claudiu T. Supuran
Article: 2189126
Published online: 23 Mar 2023
AbstractforSynthesis, biological evaluation and theoretical studies of (E)-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibitors | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1329 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

RESEARCH PAPER

Article
Design and biological evaluation of 3-substituted quinazoline-2,4(1H,3H)-dione derivatives as dual c-Met/VEGFR-2-TK inhibitors
Abdelfattah Hassan, Fawzy A. F. Mubarak, Ihsan A. Shehadi, Ahmed M. Mosallam, Hussain Temairk, Mohamed Badr & Aboubakr H. Abdelmonsef
Article: 2189578
Published online: 15 Mar 2023
AbstractforDesign and biological evaluation of 3-substituted quinazoline-2,4(1H,3H)-dione derivatives as dual c-Met/VEGFR-2-TK inhibitors | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 1864 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors
Zainab M. Elsayed, Hadia Almahli, Alessio Nocentini, Andrea Ammara, Claudiu T. Supuran, Wagdy M. Eldehna & Sahar M. Abou-Seri
Article: 2191163
Published online: 21 Mar 2023
AbstractforDevelopment of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 1244 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and anti-prion aggregation activity of acylthiosemicarbazide analogues
Dong Hwan Kim, Jaehyeon Kim, Hakmin Lee, Dongyun Lee, So Myoung Im, Ye Eun Kim, Miryeong Yoo, Yong-Pil Cheon, Jason C. Bartz, Young-Jin Son, Eun-Kyoung Choi, Yong-Sun Kim, Jae-Ho Jeon, Hyo Shin Kim, Sungeun Lee, Chongsuk Ryou & Tae-gyu Nam
Article: 2191164
Published online: 23 Mar 2023
AbstractforSynthesis and anti-prion aggregation activity of acylthiosemicarbazide analogues | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1564 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Selenium-analogs based on natural sources as cancer-associated carbonic anhydrase isoforms IX and XII inhibitors
Nora Astrain-Redin, Niccolò Paoletti, Daniel Plano, Alessandro Bonardi, Paola Gratteri, Andrea Angeli, Carmen Sanmartin & Claudiu T. Supuran
Article: 2191165
Published online: 20 Mar 2023
AbstractforSelenium-analogs based on natural sources as cancer-associated carbonic anhydrase isoforms IX and XII inhibitors | Full Text | References | PDF (2.1 MB) | EPUB
  • 1234 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and evaluation of OA-tacrine hybrids as cholinesterase inhibitors with low neurotoxicity and hepatotoxicity against Alzheimer’s disease
Huali Yang, Hongwei Jia, Minghui Deng, Kaicheng Zhang, Yaoyang Liu, Yang Liu, Maosheng Cheng & Wei Xiao
Article: 2192439
Published online: 23 Mar 2023
AbstractforDesign, synthesis and evaluation of OA-tacrine hybrids as cholinesterase inhibitors with low neurotoxicity and hepatotoxicity against Alzheimer’s disease | Full Text | References | PDF (2.7 MB) | EPUB
  • 1671 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Tripeptides conjugated with thiosemicarbazones: new inhibitors of tyrosinase for cosmeceutical use
Patrycja Ledwoń, Waldemar Goldeman, Katarzyna Hałdys, Michał Jewgiński, Greta Calamai, Joanna Rossowska, Anna Maria Papini, Paolo Rovero & Rafał Latajka
Article: 2193676
Published online: 05 May 2023
AbstractforTripeptides conjugated with thiosemicarbazones: new inhibitors of tyrosinase for cosmeceutical use | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 2108 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological evaluation of flavonoid-based IP6K2 inhibitors
Myunghwan Ahn, Seung Eun Park, Jiyeon Choi, Jiahn Choi, Doyoung Choi, Dongju An, Hayoung Jeon, Soowhan Oh, Kiho Lee, Jaehoon Kim, Jaebong Jang, Seyun Kim & Youngjoo Byun
Article: 2193866
Published online: 04 Apr 2023
AbstractforSynthesis and biological evaluation of flavonoid-based IP6K2 inhibitors | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1792 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Inhibitory effects of sulfenimides on human and bovine carbonic anhydrase enzymes
Hasan Yakan, Gürkan Bilir, Şükriye Çakmak, Ömer Taş, Nalan Türköz Karakullukçu, Ercan Soydan, Halil Kütük, Coşkun Güçlü, Murat Şentürk, Tayfun Arslan, Seyhan Öztürk, Ercüment Aksakal & Deniz Ekinci
Article: 2194573
Published online: 27 Mar 2023
AbstractforInhibitory effects of sulfenimides on human and bovine carbonic anhydrase enzymes | Full Text | References | PDF (2 MB) | EPUB
  • 1282 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and biological evaluation of novel histone deacetylase (HDAC) inhibitors derived from β-elemene scaffold
Yuan Gao, Jilong Duan, Xiawen Dang, Yinghui Yuan, Yu Wang, Xingrui He, Renren Bai, Xiang-Yang Ye & Tian Xie
Article: 2195991
Published online: 04 Apr 2023
AbstractforDesign, synthesis and biological evaluation of novel histone deacetylase (HDAC) inhibitors derived from β-elemene scaffold | Full Text | References | PDF (5.8 MB) | EPUB | Supplemental
  • 1564 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Probing mutation-induced conformational transformation of the GTP/M-RAS complex through Gaussian accelerated molecular dynamics simulations
Huayin Bao, Wei Wang, Haibo Sun & Jianzhong Chen
Article: 2195995
Published online: 14 Apr 2023
AbstractforProbing mutation-induced conformational transformation of the GTP/M-RAS complex through Gaussian accelerated molecular dynamics simulations | Full Text | References | PDF (4.9 MB) | EPUB | Supplemental
  • 1113 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors
Samar El-Kalyoubi, Samiha A. El-Sebaey, A. M. Rashad, Hanan A. AL-Ghulikah, Mostafa M. Ghorab & Sherin M. Elfeky
Article: 2198163
Published online: 10 Apr 2023
AbstractforSynthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors | Full Text | References | PDF (3.8 MB) | EPUB | Supplemental
  • 1199 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Asymmetric triplex metallohelices stabilise DNA G-quadruplexes in promoter oncogene sequences and efficiently reduce their expression in cancer cells
Jaroslav Malina, Hana Kostrhunova, Hualong Song, Peter Scott & Viktor Brabec
Article: 2198678
Published online: 05 Apr 2023
AbstractforAsymmetric triplex metallohelices stabilise DNA G-quadruplexes in promoter oncogene sequences and efficiently reduce their expression in cancer cells | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1056 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Triple targeting of mutant EGFRL858R/T790M, COX-2, and 15-LOX: design and synthesis of novel quinazolinone tethered phenyl urea derivatives for anti-inflammatory and anticancer evaluation
Hend Kothayer, Samar Rezq, Ahmed S. Abdelkhalek, Damian G. Romero & Samar S. Elbaramawi
Article: 2199166
Published online: 11 Apr 2023
AbstractforTriple targeting of mutant EGFRL858R/T790M, COX-2, and 15-LOX: design and synthesis of novel quinazolinone tethered phenyl urea derivatives for anti-inflammatory and anticancer evaluation | Full Text | References | PDF (3.8 MB) | EPUB | Supplemental
  • 1965 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access

Review

Review
Bioactivity and mechanisms of flavonoids in decreasing insulin resistance
Min Zhou, William H. Konigsberg, Canhua Hao, Yinbo Pan, Jie Sun & Xiaojing Wang
Article: 2199168
Published online: 10 Apr 2023
AbstractforBioactivity and mechanisms of flavonoids in decreasing insulin resistance | Full Text | References | PDF (1.8 MB) | EPUB
  • 2833 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Metabolomic profile, anti-trypanosomal potential and molecular docking studies of Thunbergia grandifolia
Heba A. S. El-Nashar, Ahmed M. Sayed, Hany A. M. El-Sherief, Mostafa E. Rateb, Lina Akil, Ibrahim Khadra, Taghreed A. Majrashi, Sara T. Al-Rashood, Faizah A. Binjubair, Mahmoud A. El Hassab, Wagdy M. Eldehna, Usama Ramadan Abdelmohsen & Nada M. Mostafa
Article: 2199950
Published online: 20 Apr 2023
AbstractforMetabolomic profile, anti-trypanosomal potential and molecular docking studies of Thunbergia grandifolia | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 1609 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Benzenesulfonamide derivatives as Vibrio cholerae carbonic anhydrases inhibitors: a computational-aided insight in the structural rigidity-activity relationships
Marialuigia Fantacuzzi, Ilaria D’Agostino, Simone Carradori, Francesco Liguori, Fabrizio Carta, Mariangela Agamennone, Andrea Angeli, Filomena Sannio, Jean-Denis Docquier, Clemente Capasso & Claudiu T. Supuran
Article: 2201402
Published online: 19 Apr 2023
AbstractforBenzenesulfonamide derivatives as Vibrio cholerae carbonic anhydrases inhibitors: a computational-aided insight in the structural rigidity-activity relationships | Full Text | References | PDF (4.3 MB) | EPUB | Supplemental
  • 1220 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
Effect of hydrophobic extension of aryl enaminones and pyrazole-linked compounds combined with sulphonamide, sulfaguanidine, or carboxylic acid functionalities on carbonic anhydrase inhibitory potency and selectivity
Heba Abdelrasheed Allam, Mohamed E. Albakry, Walaa R. Mahmoud, Alessandro Bonardi, Shaimaa A. Moussa, Samy Mohamady, Hatem A. Abdel-Aziz, Claudiu T. Supuran & Hany S. Ibrahim
Article: 2201403
Published online: 20 Apr 2023
AbstractforEffect of hydrophobic extension of aryl enaminones and pyrazole-linked compounds combined with sulphonamide, sulfaguanidine, or carboxylic acid functionalities on carbonic anhydrase inhibitory potency and selectivity | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 1429 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Identification of new 4-(6-oxopyridazin-1-yl)benzenesulfonamides as multi-target anti-inflammatory agents targeting carbonic anhydrase, COX-2 and 5-LOX enzymes: synthesis, biological evaluations and modelling insights
Waleed A. Badawi, Mahmoud Rashed, Alessio Nocentini, Alessandro Bonardi, Mohammad M. Abd-Alhaseeb, Sara T. Al-Rashood, Giri Babu Veerakanellore, Taghreed A. Majrashi, Eslam B. Elkaeed, Bahaa Elgendy, Paola Gratteri, Claudiu T. Supuran, Wagdy M. Eldehna & Mohamed Elagawany
Article: 2201407
Published online: 20 Apr 2023
AbstractforIdentification of new 4-(6-oxopyridazin-1-yl)benzenesulfonamides as multi-target anti-inflammatory agents targeting carbonic anhydrase, COX-2 and 5-LOX enzymes: synthesis, biological evaluations and modelling insights | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1878 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of novel benzohydroxamate-based histone deacetylase 6 (HDAC6) inhibitors with the ability to potentiate anti-PD-L1 immunotherapy in melanoma
Xiaopeng Peng, Ziwen Yu, Goverdhan Surineni, Bulian Deng, Meizhu Zhang, Chuan Li, Zhiqiang Sun, Wanyi Pan, Yao Liu, Shenglan Liu, Bin Yu & Jianjun Chen
Article: 2201408
Published online: 25 Apr 2023
AbstractforDiscovery of novel benzohydroxamate-based histone deacetylase 6 (HDAC6) inhibitors with the ability to potentiate anti-PD-L1 immunotherapy in melanoma | Full Text | References | PDF (4 MB) | EPUB | Supplemental
  • 2550 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Styrylquinazoline derivatives as ABL inhibitors selective for different DFG orientations
Katarzyna Malarz, Jacek Mularski, Marcin Pacholczyk & Robert Musiol
Article: 2201410
Published online: 18 Apr 2023
AbstractforStyrylquinazoline derivatives as ABL inhibitors selective for different DFG orientations | Full Text | References | PDF (4.7 MB) | EPUB | Supplemental
  • 859 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Design and statistical optimisation of emulsomal nanoparticles for improved anti-SARS-CoV-2 activity of N-(5-nitrothiazol-2-yl)-carboxamido candidates: in vitro and in silico studies
Ahmed A. Al-Karmalawy, Dalia S. El-Gamil, Rabeh El-Shesheny, Marwa Sharaky, Radwan Alnajjar, Omnia Kutkat, Yassmin Moatasim, Mohamed Elagawany, Sara T. Al-Rashood, Faizah A. Binjubair, Wagdy M. Eldehna, Ayman M. Noreddin & Mohamed Y. Zakaria
Article: 2202357
Published online: 24 Apr 2023
AbstractforDesign and statistical optimisation of emulsomal nanoparticles for improved anti-SARS-CoV-2 activity of N-(5-nitrothiazol-2-yl)-carboxamido candidates: in vitro and in silico studies | Full Text | References | PDF (6 MB) | EPUB | Supplemental
  • 1647 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Development of new TAK-285 derivatives as potent EGFR/HER2 inhibitors possessing antiproliferative effects against 22RV1 and PC3 prostate carcinoma cell lines
Seohyun Son, Ahmed Elkamhawy, Anam Rana Gul, Ahmed A. Al‐Karmalawy, Radwan Alnajjar, Ahmed Abdeen, Samah F. Ibrahim, Saud O. Alshammari, Qamar A. Alshammari, Won Jun Choi, Tae Jung Park & Kyeong Lee
Article: 2202358
Published online: 25 Apr 2023
AbstractforDevelopment of new TAK-285 derivatives as potent EGFR/HER2 inhibitors possessing antiproliferative effects against 22RV1 and PC3 prostate carcinoma cell lines | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
  • 2481 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of the first-in-class potent and isoform-selective human carbonic anhydrase III inhibitors
Simone Giovannuzzi, Alessandro Bonardi, Paola Gratteri, Alessio Nocentini & Claudiu T. Supuran
Article: 2202360
Published online: 24 Apr 2023
AbstractforDiscovery of the first-in-class potent and isoform-selective human carbonic anhydrase III inhibitors | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
  • 1189 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of novel thiosemicarbazone derivatives with potent and selective anti-Candida glabrata activity
Xianru Li, Liping Li, Haonan Zhang, Xiaochen Chi, Yuanying Jiang & Tingjunhong Ni
Article: 2202362
Published online: 20 Apr 2023
AbstractforDiscovery of novel thiosemicarbazone derivatives with potent and selective anti-Candida glabrata activity | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1121 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of sulfonamide-tethered isatin derivatives as novel anticancer agents and VEGFR-2 inhibitors
Moataz A. Shaldam, Hadia Almahli, Andrea Angeli, Rehab Mustafa Badi, Eman F. Khaleel, Abdelrahman I. Zain-Alabdeen, Zainab M. Elsayed, Eslam B. Elkaeed, Rofaida Salem, Claudiu T. Supuran, Wagdy M. Eldehna & Haytham O. Tawfik
Article: 2203389
Published online: 25 Apr 2023
AbstractforDiscovery of sulfonamide-tethered isatin derivatives as novel anticancer agents and VEGFR-2 inhibitors | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
  • 2191 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
A novel RRGW derived peptide is a promising inhibitor of BoNT/A
Wantong Ma, Lulu Wang, Xiangmin Tan, Xin Wang, Chunyan Yang, Yu Wang, Ziye Liu, Bo Liu, Hai Zhu, Dejuan Zhi & Dongsheng Wang
Article: 2203878
Published online: 27 Apr 2023
AbstractforA novel RRGW derived peptide is a promising inhibitor of BoNT/A | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 2022 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel Glu-based pyrazolo[3,4-d]pyrimidine analogues: design, synthesis and biological evaluation as DHFR and TS dual inhibitors
Mater Mahnashi, Mohammed Merae Alshahrani, Amer Al Ali, Abdulaziz Asiri & Mahrous A. Abou-Salim
Article: 2203879
Published online: 20 Apr 2023
AbstractforNovel Glu-based pyrazolo[3,4-d]pyrimidine analogues: design, synthesis and biological evaluation as DHFR and TS dual inhibitors | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1342 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, in silico modelling, and in vitro biological evaluation of substituted pyrazole derivatives as potential anti-skin cancer, anti-tyrosinase, and antioxidant agents
Samuel T. Boateng, Tithi Roy, Kara Torrey, Uchechi Owunna, Sergette Banang-Mbeumi, David Basnet, Eleonora Niedda, Alexis D. Alexander, Denzel El Hage, Siriki Atchimnaidu, Bolni Marius Nagalo, Dinesh Aryal, Ann Findley, Navindra P. Seeram, Tatiana Efimova, Mario Sechi, Ronald A. Hill, Hang Ma, Jean Christopher Chamcheu & Siva Murru
Article: 2205042
Published online: 15 May 2023
AbstractforSynthesis, in silico modelling, and in vitro biological evaluation of substituted pyrazole derivatives as potential anti-skin cancer, anti-tyrosinase, and antioxidant agents | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
  • 2502 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2-a]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity
Mai A. E. Mourad, Ayman Abo Elmaaty, Islam Zaki, Ahmed A. E. Mourad, Amal Hofni, Ahmed E. Khodir, Esam M. Aboubakr, Ahmed Elkamhawy, Eun Joo Roh & Ahmed A. Al-Karmalawy
Article: 2205043
Published online: 11 May 2023
AbstractforNovel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2-a]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity | Full Text | References | PDF (4.4 MB) | EPUB
  • 1870 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Curcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking
Xinyi Qiao, Lei Ye, Jialin Lu, Chengshuang Pan, Qianjin Fei, Yang Zhu, Huitao Li, Han Lin, Ren-shan Ge & Yiyan Wang
Article: 2205052
Published online: 15 May 2023
AbstractforCurcumin analogues exert potent inhibition on human and rat gonadal 3β-hydroxysteroid dehydrogenases as potential therapeutic agents: structure-activity relationship and in silico docking | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 939 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives as novel EGFRL858R/T790M inhibitors
Jianfang Fu, Jie Yu, Xiang Zhang, Yaoyao Chang, Hongze Fan, Mengzhen Dong, Mengjia Li, Yue Liu & Jinxing Hu
Article: 2205605
Published online: 27 Apr 2023
AbstractforDesign, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidine and thieno[2,3-d]pyrimidine derivatives as novel EGFRL858R/T790M inhibitors | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
  • 2093 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of novel polysubstituted N-alkyl acridone analogues as histone deacetylase isoform-selective inhibitors for cancer therapy
Ze Wang, Li Zhao, Bo Zhang, Jiahe Feng, Yule Wang, Bin Zhang, Haixiao Jin, Lijian Ding, Ning Wang & Shan He
Article: 2206581
Published online: 05 May 2023
AbstractforDiscovery of novel polysubstituted N-alkyl acridone analogues as histone deacetylase isoform-selective inhibitors for cancer therapy | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
  • 1880 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel multi-target ligands of dopamine and serotonin receptors for the treatment of schizophrenia based on indazole and piperazine scaffolds–synthesis, biological activity, and structural evaluation
Piotr Stępnicki, Olga Wronikowska-Denysiuk, Agata Zięba, Katarzyna M. Targowska-Duda, Agata Bartyzel, Martyna Z. Wróbel, Tomasz M. Wróbel, Klaudia Szałaj, Andrzej Chodkowski, Karolina Mirecka, Barbara Budzyńska, Emilia Fornal, Jadwiga Turło, Marián Castro & Agnieszka A. Kaczor
Article: 2209828
Published online: 15 May 2023
AbstractforNovel multi-target ligands of dopamine and serotonin receptors for the treatment of schizophrenia based on indazole and piperazine scaffolds–synthesis, biological activity, and structural evaluation | Full Text | References | PDF (5.7 MB) | EPUB | Supplemental
  • 1418 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological evaluation of C-4 substituted phenoxazine-bearing hydroxamic acids with potent class II histone deacetylase inhibitory activities
Jung-Chun Chu, Hui-Ju Tseng, Sung-Bau Lee, Kai-Cheng Hsu, Ling-Wei Hsin, Ru-Hao Liang, Tony Eight Lin, Nain-Chu Gao, Liang-Chieh Chen, Wan-Hsun Lu, Andrew H.-J Wang & Wei-Jan Huang
Article: 2212326
Published online: 16 May 2023
AbstractforSynthesis and biological evaluation of C-4 substituted phenoxazine-bearing hydroxamic acids with potent class II histone deacetylase inhibitory activities | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1362 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of dual S-RBD/NRP1-targeting peptides: structure-based virtual screening, synthesis, biological evaluation, and molecular dynamics simulation studies
Chunfang Hu, Ting Guo, Yunting Zou, Junyi Gao, Yi Gao, Miaomiao Niu, Yang Xia, Xiaozhou Shen & Jindong Li
Article: 2212327
Published online: 17 May 2023
AbstractforDiscovery of dual S-RBD/NRP1-targeting peptides: structure-based virtual screening, synthesis, biological evaluation, and molecular dynamics simulation studies | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 1284 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase
Ahmed H. E. Hassan, Yeon Il Oh, Chae Hyeon Lee, Yeon Ju Kim, Soo Bin Cho, Md. Maqusood Alam, Sang-Eun Park, Kyung-Sook Chung, Kyung-Tae Lee & Yong Sup Lee
Article: 2217695
Published online: 29 May 2023
AbstractforDesign, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
  • 1062 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors
Lamya H. Al-Wahaibi, Anber F. Mohammed, Fatema El-Zahraa S. Abdel Rahman, Mostafa H. Abdelrahman, Xuyuan Gu, Laurent Trembleau & Bahaa G. M. Youssif
Article: 2218602
Published online: 31 May 2023
AbstractforDesign, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1251 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Correction

Correction
Correction
Article: 2218746
Published online: 05 Jun 2023
First Page PreviewforCorrection | Full Text | PDF (2.6 MB) | EPUB
  • 326 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Short Communication

Rapid Communication
Crystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor
Masaru Goto, Natsumi Sakamoto, Shoko Higashi, Rena Kawata, Kazuki Nagatsu & Ryota Saito
Article: 2219038
Published online: 01 Jun 2023
AbstractforCrystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor | Full Text | References | PDF (1.2 MB) | EPUB
  • 686 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Recombinant ferritins for multimodal nanomedicine
Yihao Li, Haoyu Gao, Eugenie Nepovimova, Qinghua Wu, Vojtech Adam & Kamil Kuca
Article: 2219868
Published online: 01 Jun 2023
AbstractforRecombinant ferritins for multimodal nanomedicine | Full Text | References | PDF (2.5 MB) | EPUB
  • 1618 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Review Article
Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope
Mothana K. Al-Omari, Mai Elaarag, Raed M. Al-Zoubi, Ahmad R. Al-Qudimat, Ayman A. Zarour, Enas A. Al-Hurani, Zainab E. Fares, Leena M. Alkharraz, Mohanad Shkoor, Abdulilah D. Bani-Yaseen, Omar M. Aboumarzouk, Aksam Yassin & Abdulla A. Al-Ansari
Article: 2220084
Published online: 15 Jun 2023
AbstractforOrganoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope | Full Text | References | PDF (3.1 MB) | EPUB
  • 2734 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Discovery of potent heat shock protein 90 (Hsp90) inhibitors: structure-based virtual screening, molecular dynamics simulation, and biological evaluation
Yonghua Xu, Yunting Zou, Shasha Zhou, Miao-Miao Niu, Yan Zhang, Jindong Li, Zhen Xu & Li Yang
Article: 2220558
Published online: 26 Jun 2023
AbstractforDiscovery of potent heat shock protein 90 (Hsp90) inhibitors: structure-based virtual screening, molecular dynamics simulation, and biological evaluation | Full Text | References | PDF (2.9 MB) | EPUB
  • 1388 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Design, synthesis, and antitumor efficacy of novel 5-deazaflavin derivatives backed by kinase screening, docking, and ADME studies
Walaa A. Bedewy, Mosaad S. Mohamed, Ahmed M. Abdelhameed, Mohamed A. Elsawy, Mohammed Al-Muhur, Noriyuki Ashida, Ashraf N Abdalla, Tamer A. Elwaie, Tomohisa Nagamatsu & Hamed I. Ali
Article: 2220570
Published online: 21 Jun 2023
AbstractforDesign, synthesis, and antitumor efficacy of novel 5-deazaflavin derivatives backed by kinase screening, docking, and ADME studies | Full Text | References | PDF (4.4 MB) | EPUB | Supplemental
  • 1169 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Design, synthesis, docking, MD simulations, and anti-proliferative evaluation of thieno[2,3-d]pyrimidine derivatives as new EGFR inhibitors
Eman A. Sobh, Mohammed A. Dahab, Eslam B. Elkaeed, Aisha A. Alsfouk, Ibrahim M. Ibrahim, Ahmed M. Metwaly & Ibrahim H. Eissa
Article: 2220579
Published online: 08 Jun 2023
AbstractforDesign, synthesis, docking, MD simulations, and anti-proliferative evaluation of thieno[2,3-d]pyrimidine derivatives as new EGFR inhibitors | Full Text | References | PDF (7 MB) | EPUB | Supplemental
  • 1384 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Chemical composition, seasonal variation and antiaging activities of essential oil from Callistemon subulatus leaves growing in Egypt
Omyma Rabie, Heba A. S. El-Nashar, Taghreed A. Majrashi, Tarfah Al‐Warhi, Mahmoud A. El Hassab, Wagdy M. Eldehna & Nada M. Mostafa
Article: 2224944
Published online: 27 Jun 2023
AbstractforChemical composition, seasonal variation and antiaging activities of essential oil from Callistemon subulatus leaves growing in Egypt | Full Text | References | PDF (1.6 MB) | EPUB
  • 1092 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access

Rapid Communication

Rapid Communication
Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB
Yaoyao Yan, Qi Lv, Feilong Zhou, Yujie Jian, Liu Xinhua, Xing Chen & Yong Hu
Article: 2225135
Published online: 16 Jun 2023
AbstractforDiscovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 863 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
A method for the efficient evaluation of substrate-based cholinesterase imaging probes for Alzheimer’s disease
Sultan Darvesh, Scott Banfield, Maeve Dufour, Katrina L. Forrestall, Hillary Maillet, G. Andrew Reid, Dane Sands & Ian R. Pottie
Article: 2225797
Published online: 26 Jun 2023
AbstractforA method for the efficient evaluation of substrate-based cholinesterase imaging probes for Alzheimer’s disease | Full Text | References | PDF (5.1 MB) | EPUB | Supplemental
  • 1033 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Research progress on the kynurenine pathway in the prevention and treatment of Parkinson’s disease
Ping Chen & Xiaofei Geng
Article: 2225800
Published online: 29 Jun 2023
AbstractforResearch progress on the kynurenine pathway in the prevention and treatment of Parkinson’s disease | Full Text | References | PDF (1.1 MB) | EPUB
  • 1304 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Design, synthesis, and evaluation of novel benzoylhydrazone derivatives as Nur77 modulators with potent antitumor activity against hepatocellular carcinoma
Fengming He, Jun Chen, Taige Zhao, Qiaoqiong Wu, Na Yin, Xiumei Wang, Yijing Zhong, Xiaodan Guo, YingKun Qiu, Baicun Li, Meijuan Fang & Zhen Wu
Article: 2227777
Published online: 26 Jun 2023
AbstractforDesign, synthesis, and evaluation of novel benzoylhydrazone derivatives as Nur77 modulators with potent antitumor activity against hepatocellular carcinoma | Full Text | References | PDF (5.4 MB) | EPUB | Supplemental
  • 1158 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Discovery of novel 2-aminopyridine derivatives as ROS1 and ALK dual inhibitors to combat drug-resistant mutants including ROS1G2032R and ALKG1202R
Siming Liu, Chuan Huang, Chunhui Huang, Yaqi Huang, Yonghuan Yu, Guowu Wu, Fengqiu Guo, Ying Jiang, Shanhe Wan, Zhengguang Zhu, Yuanxin Tian, Jianghua Zhu & Jiajie Zhang
Article: 2227779
Published online: 22 Jun 2023
AbstractforDiscovery of novel 2-aminopyridine derivatives as ROS1 and ALK dual inhibitors to combat drug-resistant mutants including ROS1G2032R and ALKG1202R | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
  • 1030 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Rapid Communication

Rapid Communication
Discovery of 3-((3-amino-1H-indazol-4-yl)ethynyl)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide (AKE-72), a potent Pan-BCR-ABL inhibitor including the T315I gatekeeper resistant mutant
Ashraf K. El-Damasy, Hyun Ji Kim, Jung Woo Park, Yunju Nam, Wooyoung Hur, Eun-Kyoung Bang & Gyochang Keum
Article: 2228515
Published online: 20 Jul 2023
AbstractforDiscovery of 3-((3-amino-1H-indazol-4-yl)ethynyl)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide (AKE-72), a potent Pan-BCR-ABL inhibitor including the T315I gatekeeper resistant mutant | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1087 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Synthesis, antimycobacterial evaluation, and molecular docking study of 1,2,4-triazole derivatives
Meng-Yu Xia, Yu-Xiang Cai, Jun-Xian Chen, Xin Zhao, Hong-Mei Dong & Zai-Chang Yang
Article: 2229070
Published online: 29 Jun 2023
AbstractforSynthesis, antimycobacterial evaluation, and molecular docking study of 1,2,4-triazole derivatives | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 948 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Short Communication

Rapid Communication
Rational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential agents against Leishmania donovani
Ahmed H. E. Hassan, Waleed A. Bayoumi, Selwan M. El-Sayed, Trong-Nhat Phan, Yeon Ju Kim, Chae Hyeon Lee, Soo Bin Cho, Taegeun Oh, Gyeongpyo Ham, Kazem Mahmoud, Joo Hwan No & Yong Sup Lee
Article: 2229071
Published online: 29 Jun 2023
AbstractforRational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential agents against Leishmania donovani | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 844 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway
Hua Zhang, Shi-Jia Zhou, Chen-Feng Shen, Yong-Nan Zhou, Cai-Yun Wu, Meng-Yu Zhu, Qi-Meng Yu, Annoor Awadasseid, Yan-Ling Wu & Wen Zhang
Article: 2230388
Published online: 13 Jul 2023
AbstractforPD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway | Full Text | References | PDF (3.8 MB) | EPUB | Supplemental
  • 1279 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Repurposing of rabeprazole as an anti-Trypanosoma cruzi drug that targets cellular triosephosphate isomerase
Itzhel García-Torres, Ignacio De la Mora-De la Mora, Gabriel López-Velázquez, Nallely Cabrera, Luis Antonio Flores-López, Ingeborg Becker, Juliana Herrera-López, Roberto Hernández, Ruy Pérez-Montfort & Sergio Enríquez-Flores
Article: 2231169
Published online: 03 Jul 2023
AbstractforRepurposing of rabeprazole as an anti-Trypanosoma cruzi drug that targets cellular triosephosphate isomerase | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1083 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in silico insights
Abdelrahman Hamdi, Muhammad Yaseen, Wafaa A. Ewes, Mashooq Ahmad Bhat, Noha I. Ziedan, Hamed W. El-Shafey, Ahmed A. B. Mohamed, Mohamed R. Elnagar, Abdullah Haikal, Dina I. A. Othman, Abdullah A. Elgazar, Ahmed H. A. Abusabaa, Kamal S. Abdelrahman, Osama M. Soltan & Mostafa M. Elbadawi
Article: 2231170
Published online: 20 Jul 2023
AbstractforDevelopment of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in silico insights | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1632 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Development of novel salicylic acid–donepezil–rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease
Yi Zhou, Ying He, Xue Teng, Jing Mi, Jing Yang, Rongrui Wei, Wenmin Liu, Qinge Ma, Zhenghuai Tan & Zhipei Sang
Article: 2231661
Published online: 06 Jul 2023
AbstractforDevelopment of novel salicylic acid–donepezil–rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1393 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel pyrimidine Schiff bases and their selenium-containing nanoparticles as dual inhibitors of CDK1 and tubulin polymerase: design, synthesis, anti-proliferative evaluation, and molecular modelling
Samar El-Kalyoubi, Samiha A. El-Sebaey, Ahmed A. El-Sayed, Moustafa S. Abdelhamid, Fatimah Agili & Sherin M. Elfeky
Article: 2232125
Published online: 04 Jul 2023
AbstractforNovel pyrimidine Schiff bases and their selenium-containing nanoparticles as dual inhibitors of CDK1 and tubulin polymerase: design, synthesis, anti-proliferative evaluation, and molecular modelling | Full Text | References | PDF (5.2 MB) | EPUB | Supplemental
  • 1141 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Identification of sulphonamide-tethered N-((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease
Mai H. ElNaggar, Abdullah A. Elgazar, Ghada Gamal, Shimaa M. Hamed, Zainab M. Elsayed, Mohamed K. El-Ashrey, Amira Abood, Mahmoud A. El Hassab, Ahmed M. Soliman, Ramadan A. El-Domany, Farid A. Badria, Claudiu T. Supuran & Wagdy M. Eldehna
Article: 2234665
Published online: 11 Jul 2023
AbstractforIdentification of sulphonamide-tethered N-((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1643 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Carbonic anhydrase inhibitory activity of phthalimide-capped benzene sulphonamide derivatives
Deepak Shilkar, Mohd Usman Mohd Siddique, Silvia Bua, Sabina Yasmin, Mrunali Patil, Ajay Kumar Timiri, Claudiu T. Supuran & Venkatesan Jayaprakash
Article: 2235089
Published online: 13 Jul 2023
AbstractforCarbonic anhydrase inhibitory activity of phthalimide-capped benzene sulphonamide derivatives | Full Text | References | PDF (2.4 MB) | EPUB
  • 977 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Application of the Mannich reaction in the structural modification of natural products
Miao-Xia Pu, Hong-Yan Guo, Zhe-Shan Quan, Xiaoting Li & Qing-Kun Shen
Article: 2235095
Published online: 14 Jul 2023
AbstractforApplication of the Mannich reaction in the structural modification of natural products | Full Text | References | PDF (2.3 MB) | EPUB
  • 1483 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
α-Glucosidase inhibition by green, white and oolong teas: in vitro activity and computational studies
Fabio Esposito, Nicolino Pala, Mauro Carcelli, Samuel T. Boateng, Paolo S. D’Aquila, Alberto Mariani, Sandro Satta, Jean Christopher Chamcheu, Mario Sechi & Vanna Sanna
Article: 2236802
Published online: 20 Jul 2023
Abstractforα-Glucosidase inhibition by green, white and oolong teas: in vitro activity and computational studies | Full Text | References | PDF (2.4 MB) | EPUB
  • 1157 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)
Xueqin Huang, Li You, Eugenie Nepovimova, Miroslav Psotka, David Malinak, Marian Valko, Ladislav Sivak, Jan Korabecny, Zbynek Heger, Vojtech Adam, Qinghua Wu & Kamil Kuca
Article: 2237209
Published online: 24 Jul 2023
AbstractforInhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK) | Full Text | References | PDF (3.3 MB) | EPUB
  • 1988 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Rapid Communication

Rapid Communication
Microtiter plate-based chemistry and in situ screening: SuFEx-enabled lead discovery of selective AChE inhibitors
Kun Tang, Huan-Huan Li, Chengyao Wu, Shi-Long Zhang, Jian-Guo Yang, Wenjian Tang & Hua-Li Qin
Article: 2237213
Published online: 28 Jul 2023
AbstractforMicrotiter plate-based chemistry and in situ screening: SuFEx-enabled lead discovery of selective AChE inhibitors | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 776 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Discovery of novel arylamide derivatives containing piperazine moiety as inhibitors of tubulin polymerisation with potent liver cancer inhibitory activity
Xiao-Yi Shi, Huang Jiao, Jia-Kai Zhang, Xin-Yi Tian, Dan-Feng Guo, Jie Gao, Mei-Qi Jia, Jian Song, Sai-Yang Zhang, Xiang-Jing Fu & Hong-Wei Tang
Article: 2237701
Published online: 24 Jul 2023
AbstractforDiscovery of novel arylamide derivatives containing piperazine moiety as inhibitors of tubulin polymerisation with potent liver cancer inhibitory activity | Full Text | References | PDF (4.7 MB) | EPUB | Supplemental
  • 981 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and anticancer properties of celastrol derivatives involved in the inhibition of VEGF
Mingxia Song, Jiantao Wen, Yi Hua, Yangnv Zhu, Qishan Xia, Qiaoyue Guo, Yiqin Luo, Xianqing Deng & Yushan Huang
Article: 2238137
Published online: 24 Jul 2023
AbstractforSynthesis and anticancer properties of celastrol derivatives involved in the inhibition of VEGF | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 924 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Discovery and biological evaluation of novel CARM1/HDAC2 dual-targeting inhibitors with anti-prostate cancer agents
Sudong Liang, Yifei Geng, Miao-Miao Niu, Yan Zhang, Weiping He, Jindong Li, Li Yang & Zhen Xu
Article: 2241118
Published online: 01 Aug 2023
AbstractforDiscovery and biological evaluation of novel CARM1/HDAC2 dual-targeting inhibitors with anti-prostate cancer agents | Full Text | References | PDF (3.9 MB) | EPUB
  • 1287 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRWT, EGFRT790M, and EGFRL858R)
Mahmoud G. Abo Al-Hamd, Haytham O. Tawfik, Omeima Abdullah, Koki Yamaguchi, Masaharu Sugiura, Ahmed B. M. Mehany, Mervat H. El-Hamamsy & Tarek F. El-Moselhy
Article: 2241674
Published online: 07 Aug 2023
AbstractforRecruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFRWT, EGFRT790M, and EGFRL858R) | Full Text | References | PDF (5.4 MB) | EPUB | Supplemental
  • 1186 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells
Dahong Yao, Jieshu You, Xuetao Yang, Jin Zhang & Xiaojun Yao
Article: 2242601
Published online: 03 Aug 2023
AbstractforFragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells | Full Text | References | PDF (5 MB) | EPUB | Supplemental
  • 893 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Inhibition by components of Glycyrrhiza uralensis of 3CLpro and HCoV-OC43 proliferation
Jang Hoon Kim, Yea-In Park, Mok Hur, Woo Tae Park, Youn-Ho Moon, Yun-Chan Huh, Tae IL Kim, Min Hye Kang, Jong Seong Kang, Chong Woon Cho & Junsoo Park
Article: 2242704
Published online: 03 Aug 2023
AbstractforInhibition by components of Glycyrrhiza uralensis of 3CLpro and HCoV-OC43 proliferation | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 677 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers
Samar El-Kalyoubi, Mohamed M. Khalifa, Mahmoud T. Abo-Elfadl, Ahmed A. El-Sayed, Ahmed Elkamhawy, Kyeong Lee & Ahmed A. Al-Karmalawy
Article: 2242714
Published online: 18 Aug 2023
AbstractforDesign and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers | Full Text | References | PDF (5.1 MB) | EPUB | Supplemental
  • 961 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, anti-inflammatory evaluation, and molecular modelling of new coumarin-based analogs combined curcumin and other heterocycles as potential TNF-α production inhibitors via upregulating Nrf2/HO-1, downregulating AKT/mTOR signalling pathways and downregulating NF-κB in LPS induced macrophages
Lina M. A. Abdel Ghany, Botros Y. Beshay, Amal M. Youssef Moustafa, Ali Hassan Ahmed Maghrabi, Eman Hussain Khalifa Ali, Rasha Mohammed Saleem, Islam Zaki & Noha Ryad
Article: 2243551
Published online: 09 Aug 2023
AbstractforDesign, synthesis, anti-inflammatory evaluation, and molecular modelling of new coumarin-based analogs combined curcumin and other heterocycles as potential TNF-α production inhibitors via upregulating Nrf2/HO-1, downregulating AKT/mTOR signalling pathways and downregulating NF-κB in LPS induced macrophages | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1618 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Peptide foldamer-based inhibitors of the SARS-CoV-2 S protein–human ACE2 interaction
Violeta Marković, Jeelan Basha Shaik, Katarzyna Ożga, Agnieszka Ciesiołkiewicz, Juan Lizandra Perez, Ewa Rudzińska-Szostak & Łukasz Berlicki
Article: 2244693
Published online: 21 Aug 2023
AbstractforPeptide foldamer-based inhibitors of the SARS-CoV-2 S protein–human ACE2 interaction | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 987 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Semisynthesis and anti-cancer properties of novel honokiol derivatives in human nasopharyngeal carcinoma CNE-2Z cells
Bo-Han Li, Hui Ma, Jing Zhu, Jie Chen, Yi-Qun Dai, Xiao-Jing Zhang, Hong-Mei Li & Cheng-Zhu Wu
Article: 2244694
Published online: 09 Aug 2023
AbstractforSemisynthesis and anti-cancer properties of novel honokiol derivatives in human nasopharyngeal carcinoma CNE-2Z cells | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1065 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Rapid Communication

Rapid Communication
Design, synthesis and in vitro biological studies of novel triazoles with potent and broad-spectrum antifungal activity
Junhe Bao, Yumeng Hao, Tingjunhong Ni, Ruina Wang, Jiacun Liu, Xiaochen Chi, Ting Wang, Shichong Yu, Yongsheng Jin, Lan Yan, Xiaomei Li, Dazhi Zhang & Fei Xie
Article: 2244696
Published online: 08 Aug 2023
AbstractforDesign, synthesis and in vitro biological studies of novel triazoles with potent and broad-spectrum antifungal activity | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 932 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model
Alessandro Pesaresi
Article: 2245168
Published online: 14 Aug 2023
AbstractforMixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 3935 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Trafficking of carbonic anhydrase 12 and bicarbonate transporters by histamine stimulation mediates intracellular acidic scenario in lung cancer cells
Hyeong jae Kim & Jeong Hee Hong
Article: 2247181
Published online: 17 Aug 2023
AbstractforTrafficking of carbonic anhydrase 12 and bicarbonate transporters by histamine stimulation mediates intracellular acidic scenario in lung cancer cells | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 706 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and biological evaluation of thiazole/thiadiazole carboxamide scaffold-based derivatives as potential c-Met kinase inhibitors for cancer treatment
Xiang Nan, Qiu-Xu Wang, Shao-Jun Xing & Zhi-Gang Liang
Article: 2247183
Published online: 29 Aug 2023
AbstractforDesign, synthesis, and biological evaluation of thiazole/thiadiazole carboxamide scaffold-based derivatives as potential c-Met kinase inhibitors for cancer treatment | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 1147 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and evaluation of dihydro-1H-indene derivatives as novel tubulin polymerisation inhibitors with anti-angiogenic and antitumor potency
Shengtao Xu, Yijun Sun, Peng Wang, Yuchen Tan, Lei Shi & Jian Chen
Article: 2247579
Published online: 17 Aug 2023
AbstractforDesign, synthesis and evaluation of dihydro-1H-indene derivatives as novel tubulin polymerisation inhibitors with anti-angiogenic and antitumor potency | Full Text | References | PDF (3.9 MB) | EPUB | Supplemental
  • 845 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
The NMR studies of CMP inhibition of polysialylation
Bo Lu, Si-Ming Liao, Xue-Hui Liu, Shi-Jie Liang, Jun Huang, Mei Lin, Li Meng, Qing-Yan Wang, Ri-Bo Huang & Guo-Ping Zhou
Article: 2248411
Published online: 24 Aug 2023
AbstractforThe NMR studies of CMP inhibition of polysialylation | Full Text | References | PDF (1.3 MB) | EPUB
  • 661 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Aryl derivatives of 3H-1,2-benzoxaphosphepine 2-oxides as inhibitors of cancer-related carbonic anhydrase isoforms IX and XII
Anastasija Balašova, Aleksandrs Pustenko, Alessio Nocentini, Daniela Vullo, Claudiu T. Supuran & Raivis Žalubovskis
Article: 2249267
Published online: 01 Sep 2023
AbstractforAryl derivatives of 3H-1,2-benzoxaphosphepine 2-oxides as inhibitors of cancer-related carbonic anhydrase isoforms IX and XII | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 699 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of pyrimidine-tethered benzothiazole derivatives as novel anti-tubercular agents towards multi- and extensively drug resistant Mycobacterium tuberculosis
Loah R. Hemeda, Mahmoud A. El Hassab, Mohamed A. Abdelgawad, Eman F. Khaleel, Marwa M. Abdel-Aziz, Faizah A. Binjubair, Sara T. Al-Rashood, Wagdy M. Eldehna & Mohamed K. El-Ashrey
Article: 2250575
Published online: 30 Aug 2023
AbstractforDiscovery of pyrimidine-tethered benzothiazole derivatives as novel anti-tubercular agents towards multi- and extensively drug resistant Mycobacterium tuberculosis | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1025 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Insights into the inhibitory activities of neolignans and diarylnonanoid derivatives from nutmeg (Myristica fragrans Houtt.) seeds on soluble epoxide hydrolase using in vitro and in silico approaches
Vu Thi Oanh, Nguyen Viet Phong, Byung Sun Min, Seo Young Yang & Jeong Ah Kim
Article: 2251099
Published online: 28 Aug 2023
AbstractforInsights into the inhibitory activities of neolignans and diarylnonanoid derivatives from nutmeg (Myristica fragrans Houtt.) seeds on soluble epoxide hydrolase using in vitro and in silico approaches | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 1091 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Design, synthesis, biological evaluation and molecular docking study of novel pleuromutilin derivatives containing substituted benzoxazole as antibacterial agents
Jie Ren, Qi-Wen Zhang, Xian-Jin He, Xiao-Ying Chen, Zi-Dan Zhou, Zhen-Ling Zeng, Zhen Jin & You-Zhi Tang
Article: 2251712
Published online: 04 Sep 2023
AbstractforDesign, synthesis, biological evaluation and molecular docking study of novel pleuromutilin derivatives containing substituted benzoxazole as antibacterial agents | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1296 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
The hope and hype of ellagic acid and urolithins as ligands of SARS-CoV-2 Nsp5 and inhibitors of viral replication
Elisa Bianconi, Anna Gidari, Maria Souma, Samuele Sabbatini, Deborah Grifagni, Carlo Bigiotti, Elisabetta Schiaroli, Lucia Comez, Alessandro Paciaroni, Francesca Cantini, Daniela Francisci & Antonio Macchiarulo
Article: 2251721
Published online: 28 Aug 2023
AbstractforThe hope and hype of ellagic acid and urolithins as ligands of SARS-CoV-2 Nsp5 and inhibitors of viral replication | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 789 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Potent inhibition of human tyrosinase inhibitor by verproside from the whole plant of Pseudolysimachionrotundum var. subintegrum
Sunin Jung, So-Yeun Woo, Mi Hyeon Park, Doo-Young Kim, Su Ui Lee, Sei-Ryang Oh, Mun-Ock Kim, Jinhyuk Lee & Hyung Won Ryu
Article: 2252198
Published online: 30 Aug 2023
AbstractforPotent inhibition of human tyrosinase inhibitor by verproside from the whole plant of Pseudolysimachionrotundum var. subintegrum | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 795 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Targeting reversible post-translational modifications with PROTACs: a focus on enzymes modifying protein lysine and arginine residues
Marta Pichlak, Tomasz Sobierajski, Katarzyna M. Błażewska & Edyta Gendaszewska-Darmach
Article: 2254012
Published online: 04 Sep 2023
AbstractforTargeting reversible post-translational modifications with PROTACs: a focus on enzymes modifying protein lysine and arginine residues | Full Text | References | PDF (6.6 MB) | EPUB
  • 1853 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Design, synthesis, conformational analysis, and biological activity of Cα1-to-Cα6 1,4- and 4,1-disubstituted 1H-[1,2,3]triazol-1-yl-bridged oxytocin analogues
Francesca Nuti, Maud Larregola, Agnieszka Staśkiewicz, Bernhard Retzl, Nataša Tomašević, Lorenzo Macchia, Maria E. Street, Michał Jewgiński, Olivier Lequin, Rafal Latajka, Paolo Rovero, Christian W. Gruber, Michael Chorev & Anna Maria Papini
Article: 2254019
Published online: 21 Sep 2023
AbstractforDesign, synthesis, conformational analysis, and biological activity of Cα1-to-Cα6 1,4- and 4,1-disubstituted 1H-[1,2,3]triazol-1-yl-bridged oxytocin analogues | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1022 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Correction

Correction
Correction
Article: 2255447
Published online: 04 Sep 2023
CitationforCorrection | Full Text | PDF (277.1 KB) | EPUB
  • 227 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Lavandula angustifolia mill. (Lamiaceae) ethanol extract and its main constituents as promising agents for the treatment of metabolic disorders: chemical profile, in vitro biological studies, and molecular docking
Rosa Tundis, Fedora Grande, Maria A. Occhiuzzi, Vincenzo Sicari, Monica R. Loizzo & Anna R. Cappello
Article: 2269481
Published online: 18 Oct 2023
AbstractforLavandula angustifolia mill. (Lamiaceae) ethanol extract and its main constituents as promising agents for the treatment of metabolic disorders: chemical profile, in vitro biological studies, and molecular docking | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1306 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Letter to the Editor

Letter to the Editor
Oxidation of flavonoids by tyrosinase and by o-quinones–comment on "Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach” published by K. Jakimiuk, S. Sari, R. Milewski, C.T. Supuran, D. Şöhretoğlu, and M. Tomczyk (J Enzyme Inhib Med Chem 2022;37:427–436)
Hubert Wojtasek
Article: 2269611
Published online: 16 Oct 2023
CitationforOxidation of flavonoids by tyrosinase and by o-quinones–comment on "Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach” published by K. Jakimiuk, S. Sari, R. Milewski, C.T. Supuran, D. Şöhretoğlu, and M. Tomczyk (J Enzyme Inhib Med Chem 2022;37:427–436) | Full Text | References | PDF (266.7 KB) | EPUB
  • 356 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Letter to the Editor
Reply letter to Dr. Wojtasek regarding: Oxidation of flavonoids by tyrosinase and by o-quinones–comment on "Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach” published by K. Jakimiuk, S. Sari, R. Milewski, C.T. Supuran, D. Söhretoglu, and M. Tomczyk (J Enzyme Inhib Med Chem 2022;37:427-436)
Michał Tomczyk & on behalf of all co-authors
Article: 2269613
Published online: 18 Oct 2023
CitationforReply letter to Dr. Wojtasek regarding: Oxidation of flavonoids by tyrosinase and by o-quinones–comment on "Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach” published by K. Jakimiuk, S. Sari, R. Milewski, C.T. Supuran, D. Söhretoglu, and M. Tomczyk (J Enzyme Inhib Med Chem 2022;37:427-436) | Full Text | References | PDF (306.7 KB) | EPUB
  • 345 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Design, synthesis, and biological investigation of selective human carbonic anhydrase II, IX, and XII inhibitors using 7-aryl/heteroaryl triazolopyrimidines bearing a sulfanilamide scaffold
Romeo Romagnoli, Tiziano De Ventura, Stefano Manfredini, Erika Baldini, Claudiu T. Supuran, Alessio Nocentini, Andrea Brancale, Carmine Varricchio, Roberta Bortolozzi, Lorenzo Manfreda & Giampietro Viola
Article: 2270180
Published online: 18 Oct 2023
AbstractforDesign, synthesis, and biological investigation of selective human carbonic anhydrase II, IX, and XII inhibitors using 7-aryl/heteroaryl triazolopyrimidines bearing a sulfanilamide scaffold | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 939 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
2H-chromene and 7H-furo-chromene derivatives selectively inhibit tumour associated human carbonic anhydrase IX and XII isoforms
Lisa Sequeira, Simona Distinto, Rita Meleddu, Marco Gaspari, Andrea Angeli, Filippo Cottiglia, Daniela Secci, Alessia Onali, Erica Sanna, Fernanda Borges, Eugenio Uriarte, Stefano Alcaro, Claudiu T. Supuran & Elias Maccioni
Article: 2270183
Published online: 23 Oct 2023
Abstractfor2H-chromene and 7H-furo-chromene derivatives selectively inhibit tumour associated human carbonic anhydrase IX and XII isoforms | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 754 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease
Dajiang Zou, Renzheng Liu, Yangjing Lv, Jianan Guo, Changjun Zhang & Yuanyuan Xie
Article: 2270781
Published online: 13 Nov 2023
AbstractforLatest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease | Full Text | References | PDF (3.7 MB) | EPUB
  • 1321 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Fluorine and chlorine substituted adamantyl-urea as molecular tools for inhibition of human soluble epoxide hydrolase with picomolar efficacy
Vladimir V. Burmistrov, Christophe Morisseau, Dmitry V. Danilov, Boris P. Gladkikh, Vladimir S. D’yachenko, Nikolay A. Zefirov, Olga N. Zefirova, Gennady M. Butov & Bruce D. Hammock
Article: 2274797
Published online: 17 Nov 2023
AbstractforFluorine and chlorine substituted adamantyl-urea as molecular tools for inhibition of human soluble epoxide hydrolase with picomolar efficacy | Full Text | References | PDF (1.3 MB) | EPUB
  • 512 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Promising inhibition of diabetes-related enzymes and antioxidant properties of Ptilostemon casabonae leaves extract
Cinzia Sanna, Antonella Fais, Benedetta Era, Giovanna L. Delogu, Enrico Sanna, Laura Dazzi, Antonella Rosa, Arianna Marengo, Patrizia Rubiolo, Antonio De Agostini, Sonia Floris & Francesca Pintus
Article: 2274798
Published online: 31 Oct 2023
AbstractforPromising inhibition of diabetes-related enzymes and antioxidant properties of Ptilostemon casabonae leaves extract | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 814 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Biotin conjugates in targeted drug delivery: is it mediated by a biotin transporter, a yet to be identified receptor, or (an)other unknown mechanism(s)?
Ravi Tripathi, Anchala Guglani, Rujuta Ghorpade & Binghe Wang
Article: 2276663
Published online: 13 Nov 2023
AbstractforBiotin conjugates in targeted drug delivery: is it mediated by a biotin transporter, a yet to be identified receptor, or (an)other unknown mechanism(s)? | Full Text | References | PDF (1.3 MB) | EPUB
  • 1078 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Flavone-based dual PARP-Tubulin inhibitor manifesting efficacy against endometrial cancer
Sachin Sharma, Kavya Chandra, Aliva Naik, Anamika Sharma, Ram Sharma, Amandeep Thakur, Ajmer Singh Grewal, Ashwani K. Dhingra, Arnab Banerjee, Jing Ping Liou, Santosh Kumar Guru & Kunal Nepali
Article: 2276665
Published online: 02 Nov 2023
AbstractforFlavone-based dual PARP-Tubulin inhibitor manifesting efficacy against endometrial cancer | Full Text | References | PDF (4.6 MB) | EPUB | Supplemental
  • 1101 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
A novel N-heterocycles substituted oseltamivir derivatives as potent inhibitors of influenza virus neuraminidase: discovery, synthesis and biological evaluation
Jiwei Zhang, Chuanfeng Liu, Ruifang Jia, Xujie Zhang, Jian Zhang, Chiara Bertagnin, Anna Bonomini, Laura Guizzo, Yuanmin Jiang, Huinan Jia, Shuzhen Jia, Xiuli Ma, Arianna Loregian, Bing Huang, Peng Zhan & Xinyong Liu
Article: 2277135
Published online: 13 Nov 2023
AbstractforA novel N-heterocycles substituted oseltamivir derivatives as potent inhibitors of influenza virus neuraminidase: discovery, synthesis and biological evaluation | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 749 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel N-Arylmethyl-aniline/chalcone hybrids as potential VEGFR inhibitors: synthesis, biological evaluations, and molecular dynamic simulations
Hesham Haffez, Nosaiba A. Elsayed, Marwa F. Ahmed, Samar S. Fatahala, Eman F. Khaleel, Rehab Mustafa Badi, Eslam B. Elkaeed, Mahmoud A. El Hassab, Sherif F. Hammad, Wagdy M. Eldehna, Nicolas Masurier & Radwan El-Haggar
Article: 2278022
Published online: 20 Nov 2023
AbstractforNovel N-Arylmethyl-aniline/chalcone hybrids as potential VEGFR inhibitors: synthesis, biological evaluations, and molecular dynamic simulations | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 866 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
Recent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents
Ying-Hui Yuan, Nian-Dong Mao, Ji-Long Duan, Hang Zhang, Carmen Garrido, Frédéric Lirussi, Yuan Gao, Tian Xie & Xiang-Yang Ye
Article: 2279906
Published online: 13 Nov 2023
AbstractforRecent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents | Full Text | References | PDF (3.7 MB) | EPUB
  • 1538 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
Methotrexate, an anti-inflammatory drug, inhibits Hepatitis E viral replication
Akash Kumar, Preeti Hooda, Anindita Puri, Radhika Khatter, Mohammed S. Al-Dosari, Neha Sinha, Mohammad K. Parvez & Deepak Sehgal
Article: 2280500
Published online: 17 Nov 2023
AbstractforMethotrexate, an anti-inflammatory drug, inhibits Hepatitis E viral replication | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 954 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
New spiro-indeno[1,2-b]quinoxalines clubbed with benzimidazole scaffold as CDK2 inhibitors for halting non-small cell lung cancer; stereoselective synthesis, molecular dynamics and structural insights
Assem Barakat, Saeed Alshahrani, Abdullah Mohammed Al-Majid, Abdullah Saleh Alamary, Matti Haukka, Marwa M. Abu-Serie, Luis R. Domingo, Sajda Ashraf, Zaheer Ul-Haq, Mohamed S. Nafie & Mohamed Teleb
Article: 2281260
Published online: 23 Nov 2023
AbstractforNew spiro-indeno[1,2-b]quinoxalines clubbed with benzimidazole scaffold as CDK2 inhibitors for halting non-small cell lung cancer; stereoselective synthesis, molecular dynamics and structural insights | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 993 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
New pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies
Wael A. A. Fadaly, Taha H. Zidan, Nesma M. Kahk, Fatma E. A. Mohamed, Marwa M. Abdelhakeem, Rehab G. Khalil & Mohamed T. M. Nemr
Article: 2281262
Published online: 27 Nov 2023
AbstractforNew pyrazolyl-thiazolidinone/thiazole derivatives as celecoxib/dasatinib analogues with selective COX-2, HER-2 and EGFR inhibitory effects: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis, molecular modelling and ADME studies | Full Text | References | PDF (5.2 MB) | EPUB | Supplemental
  • 962 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
New dammarane-type triterpenoids from hydrolyzate of total Gynostemma pentaphyllum saponins with protein tyrosine phosphatase 1B inhibitory activity
Daopeng Tan, Jianmei Wang, Xianting Wang, Lin Qin, Yimei Du, Changkuo Zhao, Peijun Liu, Qianru Zhang, Feifei Ma, Jian Xie, Di Wu & Yuqi He
Article: 2281263
Published online: 15 Nov 2023
AbstractforNew dammarane-type triterpenoids from hydrolyzate of total Gynostemma pentaphyllum saponins with protein tyrosine phosphatase 1B inhibitory activity | Full Text | References | PDF (1.9 MB) | EPUB
  • 547 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, biological evaluation, and computational studies of N-benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activity
Nafisah M. Al-Rifai, Nemeh M. Al-Khalileh, Jalal A. Zahra, Musa I. El-Barghouthi & Fouad H. Darras
Article: 2281264
Published online: 20 Nov 2023
AbstractforSynthesis, biological evaluation, and computational studies of N-benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activity | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 636 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease
Hongtao Du, Jinzhi Song, Fang Ma, Hongxin Gao, Xinyan Zhao, Renjun Mao, Xiaolong He & Yan Yan
Article: 2281893
Published online: 15 Nov 2023
AbstractforNovel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 607 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access

Review Article

Review Article
The multifaceted nature of plant acid phosphatases: purification, biochemical features, and applications
Lokesh Sharma, Amol Kahandal, Anant Kanagare, Atul Kulkarni & Chandrakant K. Tagad
Article: 2282379
Published online: 20 Nov 2023
AbstractforThe multifaceted nature of plant acid phosphatases: purification, biochemical features, and applications | Full Text | References | PDF (1.1 MB) | EPUB
  • 1242 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access

Rapid Communication

Rapid Communication
Inhibition of pathogenic bacterial carbonic anhydrases by monothiocarbamates
Simone Giovannuzzi, Anil Kumar Marapaka, Nader S. Abutaleb, Fabrizio Carta, Hsin-Wen Liang, Alessio Nocentini, Luigi Pisano, Mohamed N. Seleem, Daniel P. Flaherty & Claudiu T. Supuran
Article: 2284119
Published online: 23 Nov 2023
AbstractforInhibition of pathogenic bacterial carbonic anhydrases by monothiocarbamates | Full Text | References | PDF (567.1 KB) | EPUB
  • 571 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Article

Article
New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFV600E and EGFR inhibitors celecoxib analogs: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis and molecular modeling study
Wael A. A. Fadaly, Mohamed T. M. Nemr, Taha H. Zidan, Fatma E. A. Mohamed, Marwa M. Abdelhakeem, Nour N. Abu Jayab, Hany A. Omar & Khaled R. A. Abdellatif
Article: 2290461
Published online: 07 Dec 2023
AbstractforNew 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAFV600E and EGFR inhibitors celecoxib analogs: design, synthesis, anti-inflammatory/anti-proliferative activities, apoptosis and molecular modeling study | Full Text | References | PDF (3.9 MB) | EPUB | Supplemental
  • 666 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Development of 10-Hydroxycamptothecin-crizotinib conjugate based on the synergistic effect on lung cancer cells
Zhen Liu, Ye Xu, Lvqian Guo, Xinran Li, Junling Gao, Weiran Xie, Lianbo Zhao, Yuou Teng, Xuejiao Li & Peng Yu
Pages: 1-11
Published online: 28 Oct 2022
AbstractforDevelopment of 10-Hydroxycamptothecin-crizotinib conjugate based on the synergistic effect on lung cancer cells | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 2473 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity
Maristela Barbosa Portela, Caroliny Mello Barboza, Eduardo Moreira da Silva, Daniel Clemente de Moraes, Renata Antoun Simão, Clara Ribeiro de Souza, Verônica da Silva Cardoso, Antônio Ferreira-Pereira, Alane Beatriz Vermelho & Claudiu T. Supuran
Pages: 1-11
Published online: 28 Nov 2022
AbstractforDentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity | Full Text | References | PDF (1.9 MB) | EPUB
  • 1179 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors
Khulood H. Oudah, Walaa R. Mahmoud, Fadi M. Awadallah, Azza T. Taher, Safinaz E.-S Abbas, Heba Abdelrasheed Allam, Daniela Vullo & Claudiu T. Supuran
Pages: 12-23
Published online: 28 Oct 2022
AbstractforDesign and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1679 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Ligand-based discovery of coronavirus main protease inhibitors using MACAW molecular embeddings
Jie Dong, Mihayl Varbanov, Stéphanie Philippot, Fanny Vreken, Wen-bin Zeng & Vincent Blay
Pages: 24-35
Published online: 28 Oct 2022
AbstractforLigand-based discovery of coronavirus main protease inhibitors using MACAW molecular embeddings | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 2204 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Unveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans
Rosa Bellavita, Annarita Falanga, Francesco Merlino, Gabriella D’Auria, Nicola Molfetta, Anella Saviano, Francesco Maione, Umberto Galdiero, Maria Rosaria Catania, Stefania Galdiero, Paolo Grieco, Emanuela Roscetto, Lucia Falcigno & Elisabetta Buommino
Pages: 36-50
Published online: 28 Oct 2022
AbstractforUnveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1633 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and discovery of the first potent proteolysis targeting chimaera (PROTAC) degrader of AIMP2-DX2 as a lung cancer drug
BoRa Lee, Dae Gyu Kim, Aram Lee, Young Mi Kim, Lianji Cui, Sunghoon Kim & Inhee Choi
Pages: 51-66
Published online: 28 Oct 2022
AbstractforSynthesis and discovery of the first potent proteolysis targeting chimaera (PROTAC) degrader of AIMP2-DX2 as a lung cancer drug | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 3559 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Prospecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed
Gerciane Silva de Oliveira, Amanda Maria de Souza Nascimento, Anna Beatriz Santana Luz, Ana Júlia Felipe Camelo Aguiar, Mayara Santa Rosa Lima, Lídia Leonize Rodrigues Matias, Isabel Rodríguez Amado, Thais Souza Passos, Karla Suzane Florentino da Silva Chaves Damasceno, Norberto de Kássio Vieira Monteiro, Susana Margarida Gomes Moreira, Lorenzo Pastrana & Ana Heloneida de Araújo Morais
Pages: 67-83
Published online: 28 Oct 2022
AbstractforProspecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1973 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Binding selectivity-dependent molecular mechanism of inhibitors towards CDK2 and CDK6 investigated by multiple short molecular dynamics and free energy landscapes
Lifei Wang, Dan Lu, Yan Wang, Xiaoyan Xu, Peihua Zhong & Zhiyong Yang
Pages: 84-99
Published online: 07 Nov 2022
AbstractforBinding selectivity-dependent molecular mechanism of inhibitors towards CDK2 and CDK6 investigated by multiple short molecular dynamics and free energy landscapes | Full Text | References | PDF (5.9 MB) | EPUB | Supplemental
  • 1968 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Article
Chromone-based monoamine oxidase B inhibitor with potential iron-chelating activity for the treatment of Alzheimer’s disease
Changjun Zhang, Yujia Zhang, Yangjing Lv, Jianan Guo, Bianbian Gao, Yi Lu, Anjie Zang, Xi Zhu, Tao Zhou & Yuanyuan Xie
Pages: 100-117
Published online: 15 Dec 2022
AbstractforChromone-based monoamine oxidase B inhibitor with potential iron-chelating activity for the treatment of Alzheimer’s disease | Full Text | References | PDF (2.8 MB) | EPUB
  • 2156 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and biological evaluation of novel ciprofloxacin derivatives as potential anticancer agents targeting topoisomerase II enzyme
Hadeer K. Swedan, Asmaa E. Kassab, Ehab M. Gedawy & Salwa E. Elmeligie
Pages: 118-137
Published online: 28 Oct 2022
AbstractforDesign, synthesis, and biological evaluation of novel ciprofloxacin derivatives as potential anticancer agents targeting topoisomerase II enzyme | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
  • 2600 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Article
Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
Miłosz Nesterowicz, Małgorzata Żendzian-Piotrowska, Jerzy Robert Ładny, Anna Zalewska & Mateusz Maciejczyk
Pages: 138-155
Published online: 02 Nov 2022
AbstractforAntiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 2362 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors
Morteza Abdoli, Alessandro Bonardi, Claudiu T. Supuran & Raivis Žalubovskis
Pages: 156-165
Published online: 28 Oct 2022
Abstractfor4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors | Full Text | References | PDF (1.8 MB) | EPUB
  • 1555 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
Discovery of dual tubulin-NEDDylation inhibitors with antiproliferative activity
Dong-Jun Fu & Ting Wang
Pages: 166-175
Published online: 04 Nov 2022
AbstractforDiscovery of dual tubulin-NEDDylation inhibitors with antiproliferative activity | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1203 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Biological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFRWT and EGFRT790M inhibitors
Tarfah Al-Warhi, Ahmed A. Al-Karmalawy, Ayman Abo Elmaaty, Maha A. Alshubramy, Marwa Abdel-Motaal, Taghreed A. Majrashi, Medhat Asem, Ahmed Nabil, Wagdy M. Eldehna & Marwa Sharaky
Pages: 176-191
Published online: 01 Nov 2022
AbstractforBiological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFRWT and EGFRT790M inhibitors | Full Text | References | PDF (4 MB) | EPUB | Supplemental
  • 4243 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Article
Identification of the first-in-class dual inhibitors of human DNA topoisomerase IIα and indoleamine-2,3-dioxygenase 1 (IDO 1) with strong anticancer properties
Barbara Kaproń, Anita Płazińska, Wojciech Płaziński & Tomasz Plech
Pages: 192-202
Published online: 08 Nov 2022
AbstractforIdentification of the first-in-class dual inhibitors of human DNA topoisomerase IIα and indoleamine-2,3-dioxygenase 1 (IDO 1) with strong anticancer properties | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 2032 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4-d]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors
Ibrahim M. Salem, Samia M. Mostafa, Ismail Salama, Osama I. El-Sabbagh, Wael A. H. Hegazy & Tarek S. Ibrahim
Pages: 203-215
Published online: 16 Nov 2022
AbstractforDesign, synthesis and antitumor evaluation of novel pyrazolo[3,4-d]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 2006 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
3H-1,2-Benzoxaphosphepine 2-oxides as selective inhibitors of carbonic anhydrase IX and XII
Aleksandrs Pustenko, Anastasija Balašova, Alessio Nocentini, Claudiu T. Supuran & Raivis Žalubovskis
Pages: 216-224
Published online: 14 Nov 2022
Abstractfor3H-1,2-Benzoxaphosphepine 2-oxides as selective inhibitors of carbonic anhydrase IX and XII | Full Text | References | PDF (2 MB) | EPUB
  • 969 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
1,2,3-Benzoxathiazine-2,2-dioxides – effective inhibitors of human carbonic anhydrases
Jekaterina Ivanova, Morteza Abdoli, Alessio Nocentini, Raivis Žalubovskis & Claudiu T. Supuran
Pages: 225-238
Published online: 13 Nov 2022
Abstractfor1,2,3-Benzoxathiazine-2,2-dioxides – effective inhibitors of human carbonic anhydrases | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1374 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR
Francesca Foschi, Annachiara Tinivella, Valentina Crippa, Luca Pinzi, Luca Mologni, Daniele Passarella & Giulio Rastelli
Pages: 239-245
Published online: 13 Nov 2022
AbstractforStructure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1981 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Novel N-methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced cardio vascular risks
John N. Philoppes, Mohamed A. Abdelgawad, Mohammed A. S. Abourehab, Mohamed Sebak, Mostafa A. Darwish & Phoebe F. Lamie
Pages: 246-266
Published online: 01 Dec 2022
AbstractforNovel N-methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced cardio vascular risks | Full Text | References | PDF (6 MB) | EPUB | Supplemental
  • 1888 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and antimicrobial activity of aminoalkyl resveratrol derivatives inspired by cationic peptides
Rubén Cebrián, Ricardo Lucas, María Victoria Fernández-Cantos, Koen Slot, Pablo Peñalver, Marta Martínez-García, Antonio Párraga-Leo, María Violante de Paz, Federico García, Oscar P. Kuipers & Juan Carlos Morales
Pages: 267-281
Published online: 04 Jan 2023
AbstractforSynthesis and antimicrobial activity of aminoalkyl resveratrol derivatives inspired by cationic peptides | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1881 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors
Tiantian Fan, Yinchun Ji, Danqi Chen, Xia Peng, Jing Ai & Bing Xiong
Pages: 282-293
Published online: 21 Nov 2022
AbstractforDesign, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1986 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors
Mostafa M. M. El-Miligy, Ahmed K. Al-Kubeisi, Mohamed G. Bekhit, Saad R. El-Zemity, Rasha A. Nassra & Aly A. Hazzaa
Pages: 294-308
Published online: 21 Nov 2022
AbstractforTowards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 1597 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
DMSO-tolerant ornithine decarboxylase (ODC) tandem assay optimised for high-throughput screening
Mingu Gordon Park, Suyeon Yellena Kim & C. Justin Lee
Pages: 309-318
Published online: 30 Nov 2022
AbstractforDMSO-tolerant ornithine decarboxylase (ODC) tandem assay optimised for high-throughput screening | Full Text | References | PDF (2.9 MB) | EPUB
  • 1733 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Spiro heterocycles bearing piperidine moiety as potential scaffold for antileishmanial activity: synthesis, biological evaluation, and in silico studies
Mounir A. A. Mohamed, Asmaa M. Kadry, Salma A. Bekhit, Mohammed A. S. Abourehab, Kikuko Amagase, Tamer M. Ibrahim, Ahmed M. M. El-Saghier & Adnan A. Bekhit
Pages: 330-342
Published online: 29 Nov 2022
AbstractforSpiro heterocycles bearing piperidine moiety as potential scaffold for antileishmanial activity: synthesis, biological evaluation, and in silico studies | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 1809 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
High-throughput discovery of novel small-molecule inhibitors of acid Ceramidase
Mazen Aseeri, José Luis Abad, Antonio Delgado, Gemma Fabriàs, Gemma Triola & Josefina Casas
Pages: 343-348
Published online: 15 Dec 2022
AbstractforHigh-throughput discovery of novel small-molecule inhibitors of acid Ceramidase | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1962 Views
  • 0 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers
I. Caroline Vaaland, Óscar López, Adrián Puerta, Miguel X. Fernandes, José M. Padrón, José G. Fernández-Bolaños, Magne O. Sydnes & Emil Lindbäck
Pages: 349-360
Published online: 01 Dec 2022
AbstractforInvestigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1451 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Review
An overview: metal-based inhibitors of urease
Wei Yang, Zhiyun Peng & Guangcheng Wang
Pages: 361-375
Published online: 29 Nov 2022
AbstractforAn overview: metal-based inhibitors of urease | Full Text | References | PDF (3.4 MB) | EPUB
  • 2359 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel piperine-carboximidamide hybrids: design, synthesis, and antiproliferative activity via a multi-targeted inhibitory pathway
Lamya H. Al-Wahaibi, Mohamed A. Mahmoud, Yaser A. Mostafa, Ali E. Raslan & Bahaa G. M. Youssif
Pages: 376-386
Published online: 30 Nov 2022
AbstractforNovel piperine-carboximidamide hybrids: design, synthesis, and antiproliferative activity via a multi-targeted inhibitory pathway | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1566 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of a fragment hit compound targeting D-Ala:D-Ala ligase of bacterial peptidoglycan biosynthesis
Matic Proj, Martina Hrast, Gregor Bajc, Rok Frlan, Anže Meden, Matej Butala & Stanislav Gobec
Pages: 387-397
Published online: 29 Nov 2022
AbstractforDiscovery of a fragment hit compound targeting D-Ala:D-Ala ligase of bacterial peptidoglycan biosynthesis | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1288 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Brief Report

Brief Report
Discovery of the SHP2 allosteric inhibitor 2-((3R,4R)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-5-(2,3-dichlorophenyl)-3-methylpyrrolo[2,1-f][1,2,4] triazin-4(3H)-one
Yanmei Luo, Jin Li, Yuliang Zong, Mengxin Sun, Wan Zheng, Jiapeng Zhu, Liu Liu & Bing Liu
Pages: 398-404
Published online: 08 Dec 2022
AbstractforDiscovery of the SHP2 allosteric inhibitor 2-((3R,4R)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-5-(2,3-dichlorophenyl)-3-methylpyrrolo[2,1-f][1,2,4] triazin-4(3H)-one | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 1973 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access

Research Paper

Article
Novel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells
Rania H. Abd El-Hameed, Mosaad S. Mohamed, Samir M. Awad, Bardes B. Hassan, Marwa Abd El-Fattah Khodair & Yara E. Mansour
Pages: 405-422
Published online: 02 Dec 2022
AbstractforNovel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 2602 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access

Explore articles

Explore the most recently published articles

The activity of pyrazolo[4,3-e][1,2,4]triazine and pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulphonamide derivatives in monolayer and spheroid breast cancer cell cultures
Anna Szymanowska et al.
Article | Published online: 3 May 2024
Open Access
Discovery of novel FGFR4 inhibitors through a build-up fragment strategy
Jihyung Kim et al.
Brief Report | Published online: 24 Apr 2024
Open Access
Targeting bacterial growth in biofilm conditions: rational design of novel inhibitors to mitigate clinical and food contamination using QSAR
Maria Galvez-Llompart et al.
Article | Published online: 23 Apr 2024
Open Access
Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells
Loredana Salerno et al.
Brief Report | Published online: 18 Apr 2024
Open Access