Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 39, Issue 1 (2024)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 39, Issue 1 (2024)

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Article
9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
Mateusz Olszewski, Maryna Stasevych, Viktor Zvarych & Natalia Maciejewska
Article: 2284113
Published online: 11 Dec 2023
Abstractfor9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases | Full Text | References | PDF (2.5 MB) | EPUB
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Article
Design, synthesis, and biological evaluation of piperazine derivatives involved in the 5-HT1AR/BDNF/PKA pathway
Hao Zhou, Mengjiao Li, Hui Liu, Zheng Liu, Xuekun Wang & Shiben Wang
Article: 2286183
Published online: 11 Dec 2023
AbstractforDesign, synthesis, and biological evaluation of piperazine derivatives involved in the 5-HT1AR/BDNF/PKA pathway | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
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Article
Discovery of LAH-1 as potent c-Met inhibitor for the treatment of non-small cell lung cancer
Lijie Sima, Zhongyuan Wang, Ling Yu, Youli Hou, Dongsheng Zhao, Bilan Luo, Weike Liao & Xinfu Liu
Article: 2286435
Published online: 11 Dec 2023
AbstractforDiscovery of LAH-1 as potent c-Met inhibitor for the treatment of non-small cell lung cancer | Full Text | References | PDF (2.1 MB) | EPUB
  • 1452 Views
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Article
Novel tetrahydronaphthalen-1-yl-phenethyl ureas: synthesis and dual antibacterial-anticancer activities
Yusuf Akbaba, Fatma Necmiye Kacı, Mehmet Enes Arslan, Süleyman Göksü, Adil Mardinoğlu & Hasan Türkez
Article: 2286925
Published online: 07 Dec 2023
AbstractforNovel tetrahydronaphthalen-1-yl-phenethyl ureas: synthesis and dual antibacterial-anticancer activities | Full Text | References | PDF (2.3 MB) | EPUB
  • 1347 Views
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Article
Evaluation of N-alkyl isatins and indoles as acetylcholinesterase and butyrylcholinesterase inhibitors
Kaitlyn N. Alcorn, Isabelle A. Oberhauser, Matthew D. Politeski & Todd J. Eckroat
Article: 2286935
Published online: 07 Dec 2023
AbstractforEvaluation of N-alkyl isatins and indoles as acetylcholinesterase and butyrylcholinesterase inhibitors | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 923 Views
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Article
3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents
Chao Wang, Yujing Zhang, Shanbo Yang, Lingyu Shi, Yutao Xiu, Yudong Wu & Hongfei Jiang
Article: 2286939
Published online: 11 Dec 2023
Abstractfor3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 989 Views
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Article
Suppression of lipopolysaccharide-induced COX-2 expression via p38MAPK, JNK, and C/EBPβ phosphorylation inhibition by furomagydarin A, a benzofuran glycoside from Magydaris pastinacea
Shiu-Wen Huang, Ming Jen Hsu, Hsiu-Chen Chen, Rita Meleddu, Simona Distinto, Elias Maccioni & Filippo Cottiglia
Article: 2287420
Published online: 07 Dec 2023
AbstractforSuppression of lipopolysaccharide-induced COX-2 expression via p38MAPK, JNK, and C/EBPβ phosphorylation inhibition by furomagydarin A, a benzofuran glycoside from Magydaris pastinacea | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 918 Views
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Article
Design and synthesis of doublecortin-like kinase 1 inhibitors and their bioactivity evaluation
Pengming Pan, Dengbo Ji, Zhongjun Li & Xiangbao Meng
Article: 2287990
Published online: 07 Dec 2023
AbstractforDesign and synthesis of doublecortin-like kinase 1 inhibitors and their bioactivity evaluation | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Article
Synthesis biological evaluation and molecular docking of isatin hybrids as anti-cancer and anti-microbial agents
Mohammad Altamimi, Saeed Ali Syed, Burak Tuzun, Mohammad Rashid Alhazani, Osamah Alnemer & Ahmed Bari
Article: 2288548
Published online: 11 Dec 2023
AbstractforSynthesis biological evaluation and molecular docking of isatin hybrids as anti-cancer and anti-microbial agents | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 2335 Views
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Article
Anti-cancer activity and cellular uptake of 7,3′,4′- and 7,8,4′-trihydroxyisoflavone in HepG2 cells under hypoxic conditions
Wen-Sheng Tzeng, Wei-Lin Teng, Pao-Hsien Huang, Feng-Lin Yen & Yow-Ling Shiue
Article: 2288806
Published online: 28 Dec 2023
AbstractforAnti-cancer activity and cellular uptake of 7,3′,4′- and 7,8,4′-trihydroxyisoflavone in HepG2 cells under hypoxic conditions | Full Text | References | PDF (2.9 MB) | EPUB
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Article
Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach
Keting Li, Wenshu Hu, Yingjie Wang, Wenxing Chen, Hongmei Wen, Jian Liu, Wei Li & Bo Wang
Article: 2288810
Published online: 07 Dec 2023
AbstractforSearching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1704 Views
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Article
Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies
Zorana Ferjancic, Filip Bihelovic, Bojan Vulovic, Radomir Matovic, Milena Trmcic, Aleksandar Jankovic, Milos Pavlovic, Filip Djurkovic, Radivoje Prodanovic, Aleksandra Djurdjevic Djelmas, Nevena Kalicanin, Mario Zlatovic, Dusan Sladic, Thomas Vallet, Marco Vignuzzi & Radomir N. Saicic
Article: 2289007
Published online: 12 Dec 2023
AbstractforDevelopment of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
  • 1586 Views
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Article
Novel dual-targeting inhibitors of NSD2 and HDAC2 for the treatment of liver cancer: structure-based virtual screening, molecular dynamics simulation, and in vitro and in vivo biological activity evaluations
Xing Jin, Yuting Wang, Jing Chen, Miaomiao Niu, Yang Yang, Qiaoxuan Zhang & Guangyu Bao
Article: 2289355
Published online: 07 Dec 2023
AbstractforNovel dual-targeting inhibitors of NSD2 and HDAC2 for the treatment of liver cancer: structure-based virtual screening, molecular dynamics simulation, and in vitro and in vivo biological activity evaluations | Full Text | References | PDF (3.1 MB) | EPUB
  • 1954 Views
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Article
Identification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation
Chunqiong Li, Quanjun Yang & Li Zhang
Article: 2290458
Published online: 07 Dec 2023
AbstractforIdentification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1473 Views
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Research Paper

Article
Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
Karol Biernacki, Olga Ciupak, Mateusz Daśko, Janusz Rachon, Damian Flis, Justyna Budka, Iwona Inkielewicz-Stępniak, Anna Czaja, Janusz Rak & Sebastian Demkowicz
Article: 2290910
Published online: 13 Dec 2023
AbstractforDevelopment of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19 | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 1258 Views
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Review Article

Review Article
Glutaminase inhibition as potential cancer therapeutics: current status and future applications
Rajath Cyriac & Kwangho Lee
Article: 2290911
Published online: 11 Dec 2023
AbstractforGlutaminase inhibition as potential cancer therapeutics: current status and future applications | Full Text | References | PDF (1.2 MB) | EPUB
  • 2327 Views
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Research Paper

Article
Ligand-based pharmacophore modelling, structure optimisation, and biological evaluation for the identification of 2-heteroarylthio-N-arylacetamides as novel HSP90 C-terminal inhibitors
Yajun Liu, Chenyao Li, Yajing Li, Shuming Zhang, Ning Zhang, Xiaobo Bian & Shutao Tan
Article: 2290912
Published online: 11 Dec 2023
AbstractforLigand-based pharmacophore modelling, structure optimisation, and biological evaluation for the identification of 2-heteroarylthio-N-arylacetamides as novel HSP90 C-terminal inhibitors | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1282 Views
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Review Article

Review Article
Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship
Dimitrios Tsikas
Article: 2291336
Published online: 11 Dec 2023
AbstractforAcetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship | Full Text | References | PDF (1.8 MB) | EPUB
  • 2375 Views
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Research Article

Article
Novel isobavachalcone derivatives induce apoptosis and necroptosis in human non-small cell lung cancer H1975 cells
Jie Chen, Long Zhao, Meng-Fan Xu, Di Huang, Xiao-Long Sun, Yu-Xin Zhang, Hong-Mei Li & Cheng-Zhu Wu
Article: 2292006
Published online: 12 Dec 2023
AbstractforNovel isobavachalcone derivatives induce apoptosis and necroptosis in human non-small cell lung cancer H1975 cells | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 1737 Views
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Article
Comparative metabolic study of the chloroform fraction of three Cystoseira species based on UPLC/ESI/MS analysis and biological activities
Shaza H. Aly, Ahmed M. Elissawy, Mahmoud A. El Hassab, Taghreed A. Majrashi, Fatma E. Hassan, Eslam B. Elkaeed, Wagdy M. Eldehna & Abdel Nasser B. Singab
Article: 2292482
Published online: 12 Dec 2023
AbstractforComparative metabolic study of the chloroform fraction of three Cystoseira species based on UPLC/ESI/MS analysis and biological activities | Full Text | References | PDF (2 MB) | EPUB | Supplemental
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Article
A multidisciplinary approach to the antioxidant and hepatoprotective activities of Arbutus pavarii Pampan fruit; in vitro and in Vivo biological evaluations, and in silico investigations
Fatma A. Elshibani, Abdullah D. Alamami, Hamdoon A. Mohammed, Rabab Ahmed Rasheed, Radwa M. El Sabban, Mohamed A. Yehia, Sherif S. Abdel Mageed, Taghreed A. Majrashi, Eslam B. Elkaeed, Mahmoud A. El Hassab, Wagdy M. Eldehna & Mohamed K. El-Ashrey
Article: 2293639
Published online: 28 Dec 2023
AbstractforA multidisciplinary approach to the antioxidant and hepatoprotective activities of Arbutus pavarii Pampan fruit; in vitro and in Vivo biological evaluations, and in silico investigations | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
  • 1704 Views
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Research Paper

Article
Discovery of novel and potent dual-targeting AXL/HDAC2 inhibitors for colorectal cancer treatment via structure-based pharmacophore modelling, virtual screening, and molecular docking, molecular dynamics simulation studies, and biological evaluation
Xiao Qiao, Xiangyu Wu, Shutong Chen, Miao-Miao Niu, Huilian Hua & Yan Zhang
Article: 2295241
Published online: 22 Dec 2023
AbstractforDiscovery of novel and potent dual-targeting AXL/HDAC2 inhibitors for colorectal cancer treatment via structure-based pharmacophore modelling, virtual screening, and molecular docking, molecular dynamics simulation studies, and biological evaluation | Full Text | References | PDF (3.3 MB) | EPUB
  • 1958 Views
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Research Article

Article
Isolation, structure modification, and anti-rheumatoid arthritis activity of isopimarane-type diterpenoids from Orthosiphon aristatus
Yong-Xin Luo, Xu Gong, Zhi-Cheng Su, Jin-Feng Mo, Dong-Li Li, Ri-Hui Wu, Jing-Wei Jin, Ming Lang, Jin-Ping Wang, Xue-Tao Xu & Li-She Gan
Article: 2296355
Published online: 17 Jan 2024
AbstractforIsolation, structure modification, and anti-rheumatoid arthritis activity of isopimarane-type diterpenoids from Orthosiphon aristatus | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1041 Views
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Article
Dihydroartemisinin enhances the anti-tumour effect of photodynamic therapy by targeting PKM2-mediated glycolysis in oesophageal cancer cell
Mengru Jin, Luyao Shi, Li Wang, Dingyuan Zhang & Yanjing Li
Article: 2296695
Published online: 18 Dec 2023
AbstractforDihydroartemisinin enhances the anti-tumour effect of photodynamic therapy by targeting PKM2-mediated glycolysis in oesophageal cancer cell | Full Text | References | PDF (1.9 MB) | EPUB
  • 1285 Views
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Correction

Correction
Correction
Article: 2297117
Published online: 21 Dec 2023
CitationforCorrection | Full Text | PDF (149.5 KB) | EPUB
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Research Article

Article
Development of novel ALOX15 inhibitors combining dual machine learning filtering and fragment substitution optimisation approaches, molecular docking and dynamic simulation methods
Yinglin Liao, Peng Cao & Lianxiang Luo
Article: 2301756
Published online: 12 Jan 2024
AbstractforDevelopment of novel ALOX15 inhibitors combining dual machine learning filtering and fragment substitution optimisation approaches, molecular docking and dynamic simulation methods | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1471 Views
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Article
Computational fragment-based drug design of potential Glo-I inhibitors
Roaa S. Bibars & Qosay A. Al-Balas
Article: 2301758
Published online: 22 Jan 2024
AbstractforComputational fragment-based drug design of potential Glo-I inhibitors | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 664 Views
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Research Paper

Article
Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase
Elisa Rojas-Prats, Loreto Martinez-Gonzalez, Carmen Gil, David Ramírez & Ana Martinez
Article: 2301767
Published online: 11 Jan 2024
AbstractforDruggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 772 Views
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Research Article

Article
Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test
Mengfan Zhu, Jinfeng Qu & Qi Deng
Article: 2301768
Published online: 17 Jan 2024
AbstractforIdentification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 727 Views
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Article
Identification and evaluation of antiviral activity of novel compounds targeting SARS-CoV-2 virus by enzymatic and antiviral assays, and computational analysis
Ivana Nemčovičová, Katarína Lopušná, Iveta Štibrániová, Fabio Benedetti, Federico Berti, Fulvia Felluga, Sara Drioli, Mattia Vidali, Jaroslav Katrlík, Lucia Pažitná, Alena Holazová, Jana Blahutová, Simona Lenhartová, Monika Sláviková, Boris Klempa, Miroslav Ondrejovič, Daniela Chmelová, Barbora Legerská, Stanislav Miertuš, Mária Klacsová, Daniela Uhríková, Lukáš Kerti & Vladimír Frecer
Article: 2301772
Published online: 14 Jan 2024
AbstractforIdentification and evaluation of antiviral activity of novel compounds targeting SARS-CoV-2 virus by enzymatic and antiviral assays, and computational analysis | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1180 Views
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Article
Design, synthesis, and bioevaluation of 1h-pyrrolo[3,2-c]pyridine derivatives as colchicine-binding site inhibitors with potent anticancer activities
Chao Wang, Yujing Zhang, Shanbo Yang, Lingyu Shi, Rong Rong, Tingting Zhang, Yudong Wu & Dongming Xing
Article: 2302320
Published online: 14 Jan 2024
AbstractforDesign, synthesis, and bioevaluation of 1h-pyrrolo[3,2-c]pyridine derivatives as colchicine-binding site inhibitors with potent anticancer activities | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1051 Views
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Article
Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
Mateusz Olszewski, Natalia Maciejewska, Anoop Kallingal, Agnieszka Chylewska, Aleksandra M. Dąbrowska, Małgorzata Biedulska, Mariusz Makowski, José M. Padrón & Maciej Baginski
Article: 2302920
Published online: 14 Jan 2024
AbstractforPalindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 820 Views
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Article
Imparting aromaticity to 2-pyridone derivatives by O-alkylation resulted in new competitive and non-competitive PIM-1 kinase inhibitors with caspase-activated apoptosis
Marwa E. Abdelaziz, Mostafa M. M. El-Miligy, Salwa M. Fahmy, Marwa M. Abu-Serie, Aly A. Hazzaa & Mona A. Mahran
Article: 2304044
Published online: 17 Jan 2024
AbstractforImparting aromaticity to 2-pyridone derivatives by O-alkylation resulted in new competitive and non-competitive PIM-1 kinase inhibitors with caspase-activated apoptosis | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 1112 Views
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Article
Design, synthesis, molecular modelling and biological evaluation of novel 6-amino-5-cyano-2-thiopyrimidine derivatives as potent anticancer agents against leukemia and apoptotic inducers
Naglaa M. Ahmed, Mosaad S. Mohamed, Samir M. Awad, Neama A. Abd El-tawab, Mohamed S. Gaballah & Ahmed M. Said
Article: 2304625
Published online: 13 Feb 2024
AbstractforDesign, synthesis, molecular modelling and biological evaluation of novel 6-amino-5-cyano-2-thiopyrimidine derivatives as potent anticancer agents against leukemia and apoptotic inducers | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1247 Views
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Article
Boronic acid inhibitors of penicillin-binding protein 1b: serine and lysine labelling agents
Levente Kollár, Katarina Grabrijan, Martina Hrast Rambaher, Krištof Bozovičar, Tímea Imre, György G. Ferenczy, Stanislav Gobec & György M. Keserű
Article: 2305833
Published online: 27 Feb 2024
AbstractforBoronic acid inhibitors of penicillin-binding protein 1b: serine and lysine labelling agents | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 796 Views
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Article
Discovery of novel and potent CDK8 inhibitors for the treatment of acute myeloid leukaemia
Zhuoying Chen, Quan Wang, Yao Yao Yan, Dalong Jin, Yumeng Wang, Xing Xing Zhang & Xin Hua Liu
Article: 2305852
Published online: 23 Jan 2024
AbstractforDiscovery of novel and potent CDK8 inhibitors for the treatment of acute myeloid leukaemia | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 1125 Views
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Article
Design, synthesis, and apoptotic antiproliferative action of new 1,2,3-triazole/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors
Mohamed A. Mahmoud, Anber F. Mohammed, Ola I. A. Salem, Tahani Mazyad Almutairi, Stefan Bräse & Bahaa G. M. Youssif
Article: 2305856
Published online: 07 Feb 2024
AbstractforDesign, synthesis, and apoptotic antiproliferative action of new 1,2,3-triazole/1,2,4-oxadiazole hybrids as dual EGFR/VEGFR-2 inhibitors | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 985 Views
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Article
Discovery of new thymol-3,4-disubstituted thiazole hybrids as dual COX-2/5-LOX inhibitors with in vivo proof
Mostafa M. M. El-Miligy, Ahmed K. Al-Kubeisi, Rasha A. Nassra, Saad R. El-Zemity & Aly A. Hazzaa
Article: 2309171
Published online: 30 Jan 2024
AbstractforDiscovery of new thymol-3,4-disubstituted thiazole hybrids as dual COX-2/5-LOX inhibitors with in vivo proof | Full Text | References | PDF (4.4 MB) | EPUB
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Article
Development of certain benzylidene coumarin derivatives as anti-prostate cancer agents targeting EGFR and PI3Kβ kinases
Lina M. A. Abdel Ghany, Tarek S. Ibrahim, Abdulrahman S. Alharbi, Mohamed S. Abdel-Aziz, Eman M. El-labbad, Mohamed Elagawany & Noha Ryad
Article: 2311157
Published online: 13 Feb 2024
AbstractforDevelopment of certain benzylidene coumarin derivatives as anti-prostate cancer agents targeting EGFR and PI3Kβ kinases | Full Text | References | PDF (4.3 MB) | EPUB | Supplemental
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Article
New imidazole-2-thiones linked to acenaphythylenone as dual DNA intercalators and topoisomerase II inhibitors: structural optimization, docking, and apoptosis studies
Asmaa H. Mohamed, Mohammed B. Alshammari, Ashraf A. Aly, Kamal U. Sadek, Akil Ahmad, Eman A. Aziz, Amira F. El-Yazbi, Eman J. El-Agroudy & Marwa E. Abdelaziz
Article: 2311818
Published online: 15 Mar 2024
AbstractforNew imidazole-2-thiones linked to acenaphythylenone as dual DNA intercalators and topoisomerase II inhibitors: structural optimization, docking, and apoptosis studies | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 812 Views
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Article
o-Vanillin binds covalently to MAL/TIRAP Lys-210 but independently inhibits TLR2
Md. Habibur Rahaman, Sara J. Thygesen, Michael J. Maxwell, Hyoyoung Kim, Prerna Mudai, Jeffrey D. Nanson, Xinying Jia, Parimala R. Vajjhala, Andrew Hedger, Irina Vetter, Thomas Haselhorst, Avril A. B. Robertson, Brian Dymock, Thomas Ve, Mehdi Mobli, Katryn J. Stacey & Bostjan Kobe
Article: 2313055
Published online: 28 Feb 2024
Abstractforo-Vanillin binds covalently to MAL/TIRAP Lys-210 but independently inhibits TLR2 | Full Text | References | PDF (7.7 MB) | EPUB | Supplemental
  • 893 Views
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Research Paper

Article
Novel anti-neuroinflammatory pyranone-carbamate derivatives as selective butyrylcholinesterase inhibitors for treating Alzheimer’s disease
Chuanyu Yu, Xueyan Liu, Bingxiang Ma, Jiexin Xu, Yiquan Chen, Chaoxian Dai, Huaping Peng & Daijun Zha
Article: 2313682
Published online: 16 Feb 2024
AbstractforNovel anti-neuroinflammatory pyranone-carbamate derivatives as selective butyrylcholinesterase inhibitors for treating Alzheimer’s disease | Full Text | References | PDF (5.9 MB) | EPUB | Supplemental
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Research Article

Article
Design, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o-methoxy phenyl group as potential agents against gastric cancer
Xin Gan, Yuna Wu, Min Zhu, Bo Liu, Miaomiao Kong, Zixuan Xi, Ke Li, Haibao Wang, Tiande Su, Jiali Yao, Fatehi Khushafah, Baozhu Yi, Jiabing Wang, Wulan Li & Jianzhang Wu
Article: 2314233
Published online: 22 Feb 2024
AbstractforDesign, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o-methoxy phenyl group as potential agents against gastric cancer | Full Text | References | PDF (5.1 MB) | EPUB | Supplemental
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Article
Design, synthesis, in vitro and in vivo biological evaluation of pterostilbene derivatives for anti-inflammation therapy
Liuzeng Chen, Ke Wang, Xiaohan Liu, Lifan Wang, Hui Zou, Shuying Hu, Lingling Zhou, Rong Li, Shiying Cao, Banfeng Ruan & Quanren Cui
Article: 2315227
Published online: 29 Feb 2024
AbstractforDesign, synthesis, in vitro and in vivo biological evaluation of pterostilbene derivatives for anti-inflammation therapy | Full Text | References | PDF (7.1 MB) | EPUB | Supplemental
  • 987 Views
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Article
Discovery of novel anaplastic lymphoma kinase (ALK) and histone deacetylase (HDAC) dual inhibitors exhibiting antiproliferative activity against non-small cell lung cancer
Kang-Li Wang, Tsung-Yu Yeh, Pei-Chen Hsu, Tzu-Hsuan Wong, Jia-Rong Liu, Ji-Wang Chern, Miao-Hsia Lin & Chao-Wu Yu
Article: 2318645
Published online: 11 Mar 2024
AbstractforDiscovery of novel anaplastic lymphoma kinase (ALK) and histone deacetylase (HDAC) dual inhibitors exhibiting antiproliferative activity against non-small cell lung cancer | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
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Review Article

Review Article
Elucidation of critical chemical moieties of metallo-β-lactamase inhibitors and prioritisation of target metallo-β-lactamases
Jung Hun Lee, Sang-Gyu Kim, Kyung-Min Jang, Kyoungmin Shin, Hyeonku Jin, Dae-Wi Kim, Byeong Chul Jeong & Sang Hee Lee
Article: 2318830
Published online: 15 Mar 2024
AbstractforElucidation of critical chemical moieties of metallo-β-lactamase inhibitors and prioritisation of target metallo-β-lactamases | Full Text | References | PDF (8.1 MB) | EPUB | Supplemental
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Research Article

Article
Targeting bacterial growth in biofilm conditions: rational design of novel inhibitors to mitigate clinical and food contamination using QSAR
Maria Galvez-Llompart, Jesús Hierrezuelo, Mariluz Blasco, Riccardo Zanni, Jorge Galvez, Antonio de Vicente, Alejandro Pérez-García & Diego Romero
Article: 2330907
Published online: 23 Apr 2024
AbstractforTargeting bacterial growth in biofilm conditions: rational design of novel inhibitors to mitigate clinical and food contamination using QSAR | Full Text | References | PDF (7 MB) | EPUB | Supplemental
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Article
Synthesis, carbonic anhydrase inhibition studies and modelling investigations of phthalimide–hydantoin hybrids
Morteza Abdoli, Alessandro Bonardi, Paola Gratteri, Claudiu T. Supuran & Raivis Žalubovskis
Article: 2335927
Published online: 12 Apr 2024
AbstractforSynthesis, carbonic anhydrase inhibition studies and modelling investigations of phthalimide–hydantoin hybrids | Full Text | References | PDF (5.6 MB) | EPUB
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Brief Report

Brief Report
Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells
Loredana Salerno, Antonietta Notaro, Valeria Consoli, Federica Affranchi, Valeria Pittalà, Valeria Sorrenti, Luca Vanella, Michela Giuliano & Sebastiano Intagliata
Article: 2337191
Published online: 18 Apr 2024
AbstractforEvaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells | Full Text | References | PDF (2.9 MB) | EPUB
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Brief Report
Discovery of novel FGFR4 inhibitors through a build-up fragment strategy
Jihyung Kim, Chang Gyun Im, Kyujin Oh, Ji Min Lee, Fatimah Al-Rubaye & Kyung Hoon Min
Article: 2343350
Published online: 24 Apr 2024
AbstractforDiscovery of novel FGFR4 inhibitors through a build-up fragment strategy | Full Text | References | PDF (1.5 MB) | EPUB
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Research Article

Article
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, Dominika Radomska, Robert Czarnomysy, Mariusz Mojzych, Katarzyna Kotwica-Mojzych, Krzysztof Bielawski & Anna Bielawska
Article: 2343352
Published online: 03 May 2024
AbstractforThe 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 | Full Text | References | PDF (8 MB) | EPUB | Supplemental
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