Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 35, Issue 1 (2020)

Browse this journal
Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days

Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 35, Issue 1 (2020)

See all volumes and issues
Vol 39, 2024 Vol 38, 2023 Vol 37, 2022 Vol 36, 2021 Volume 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

 

Article
Synthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease
Chhabi Lal Chaudhary, Pallavi Gurung, Seoul Jang, Suhrid Banskota, Tae-Gyu Nam, Jung-Ae Kim & Byeong-Seon Jeong
Pages: 1-20
Published online: 16 Oct 2019
AbstractforSynthesis, activity and mechanism of alkoxy-, carbamato-, sulfonamido-, thioureido-, and ureido-derivatives of 2,4,5-trimethylpyridin-3-ol against inflammatory bowel disease | Full Text | References | PDF (2.9 MB) | EPUB
  • 6070 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
A structure-based approach towards the identification of novel antichagasic compounds: Trypanosoma cruzi carbonic anhydrase inhibitors
Manuel A. Llanos, María L. Sbaraglini, María L. Villalba, María D. Ruiz, Carolina Carrillo, Catalina Alba Soto, Alan Talevi, Andrea Angeli, Seppo Parkkila, Claudiu T. Supuran & Luciana Gavernet
Pages: 21-30
Published online: 16 Oct 2019
AbstractforA structure-based approach towards the identification of novel antichagasic compounds: Trypanosoma cruzi carbonic anhydrase inhibitors | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 2205 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Synthesis of thiazolidin-4-ones and thiazinan-4-ones from 1-(2-aminoethyl)pyrrolidine as acetylcholinesterase inhibitors
Adriana M. das Neves, Gabriele A. Berwaldt, Cinara T. Avila, Taís B. Goulart, Bruna C. Moreira, Taís P. Ferreira, Mayara S. P. Soares, Nathalia S. Pedra, Luiza Spohr, Anita A. A. dE Souza, Roselia M. Spanevello & Wilson Cunico
Pages: 31-41
Published online: 23 Oct 2019
AbstractforSynthesis of thiazolidin-4-ones and thiazinan-4-ones from 1-(2-aminoethyl)pyrrolidine as acetylcholinesterase inhibitors | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 2399 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Enzyme-assisted modification of flavonoids from Matricaria chamomilla: antioxidant activity and inhibitory effect on digestive enzymes
Elida Paula Dini de Franco, Fabiano Jares Contesini, Bianca Lima da Silva, Anna Maria Alves de Piloto Fernandes, Camila Wielewski Leme, João Pedro Gonçalves Cirino, Paula Renata Bueno Campos & Patrícia de Oliveira Carvalho
Pages: 42-49
Published online: 28 Oct 2019
AbstractforEnzyme-assisted modification of flavonoids from Matricaria chamomilla: antioxidant activity and inhibitory effect on digestive enzymes | Full Text | References | PDF (814.6 KB) | EPUB
  • 3585 Views
  • 23 CrossRef citations
  • 0Altmetric
Open Access
Article
Optimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists
Yuanying Fang, Shaokun Zhang, Min Li, Lijuan Xiong, Liangxing Tu, Saisai Xie, Yi Jin, Yanhua Liu, Zunhua Yang & Ronghua Liu
Pages: 50-58
Published online: 28 Oct 2019
AbstractforOptimisation of novel 4, 8-disubstituted dihydropyrimido[5,4-b][1,4]oxazine derivatives as potent GPR 119 agonists | Full Text | References | PDF (1.5 MB) | EPUB
  • 1552 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Phosphonamidates are the first phosphorus-based zinc binding motif to show inhibition of β-class carbonic anhydrases from bacteria, fungi, and protozoa
Siham A. Alissa, Hanan A. Alghulikah, Zeid A. Alothman, Sameh M. Osman, Sonia Del Prete, Clemente Capasso, Alessio Nocentini & Claudiu T. Supuran
Pages: 59-64
Published online: 30 Oct 2019
AbstractforPhosphonamidates are the first phosphorus-based zinc binding motif to show inhibition of β-class carbonic anhydrases from bacteria, fungi, and protozoa | Full Text | References | PDF (995.5 KB)
  • 1596 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
In vitro inhibition of Mycobacterium tuberculosis β-carbonic anhydrase 3 with Mono- and dithiocarbamates and evaluation of their toxicity using zebrafish developing embryos
Ashok Aspatwar, Milka Hammaren, Mataleena Parikka, Seppo Parkkila, Fabrizio Carta, Murat Bozdag, Daniela Vullo & Claudiu T. Supuran
Pages: 65-71
Published online: 30 Oct 2019
AbstractforIn vitro inhibition of Mycobacterium tuberculosis β-carbonic anhydrase 3 with Mono- and dithiocarbamates and evaluation of their toxicity using zebrafish developing embryos | Full Text | References | PDF (1.2 MB) | EPUB
  • 1908 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and biological evaluation of novel 1H-1,2,4-triazole, benzothiazole and indazole-based derivatives as potent FGFR1 inhibitors viafragment-based virtual screening
Jian Liu, Yu Wen, Lina Gao, Liang Gao, Fengjun He, Jingxian Zhou, Junwei Wang, Rupeng Dai, Xiaojing Chen, Di Kang & Lihong Hu
Pages: 72-84
Published online: 04 Nov 2019
AbstractforDesign, synthesis and biological evaluation of novel 1H-1,2,4-triazole, benzothiazole and indazole-based derivatives as potent FGFR1 inhibitors viafragment-based virtual screening | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 2879 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery and evaluation of novel synthetic 5-alkyl-4-oxo-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoxaline-1-carbox-amide derivatives as anti-inflammatory agents
Qing-Kun Shen, Guo-Hua Gong, Gao- Li, Mei- Jin, Li-Hua Cao & Zhe-Shan Quan
Pages: 85-95
Published online: 11 Nov 2019
AbstractforDiscovery and evaluation of novel synthetic 5-alkyl-4-oxo-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoxaline-1-carbox-amide derivatives as anti-inflammatory agents | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 2132 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access
Article
Structure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors
Suresh Velnati, Alberto Massarotti, Annamaria Antona, Maria Talmon, Luigia Grazia Fresu, Alessandra Silvia Galetto, Daniela Capello, Alessandra Bertoni, Valentina Mercalli, Andrea Graziani, Gian Cesare Tron & Gianluca Baldanzi
Pages: 96-108
Published online: 05 Nov 2019
AbstractforStructure activity relationship studies on Amb639752: toward the identification of a common pharmacophoric structure for DGKα inhibitors | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 2885 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, in vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series
Ashok Aspatwar, Nanda Kumar Parvathaneni, Harlan Barker, Emilie Anduran, Claudiu T. Supuran, Ludwig Dubois, Philippe Lambin, Seppo Parkkila & Jean-Yves Winum
Pages: 109-117
Published online: 05 Nov 2019
AbstractforDesign, synthesis, in vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 2231 Views
  • 19 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and evaluation of quinolinone derivatives containing dithiocarbamate moiety as multifunctional AChE inhibitors for the treatment of Alzheimer’s disease
Jie Fu, Fengqi Bao, Min Gu, Jing Liu, Zhipeng Zhang, Jiaoli Ding, Sai-Sai Xie & Jinsong Ding
Pages: 118-128
Published online: 07 Nov 2019
AbstractforDesign, synthesis and evaluation of quinolinone derivatives containing dithiocarbamate moiety as multifunctional AChE inhibitors for the treatment of Alzheimer’s disease | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 3259 Views
  • 30 CrossRef citations
  • 0Altmetric
Open Access
Article
Statins interfere with the attachment of S. cerevisiae mtDNA to the inner mitochondrial membrane
Angela Cirigliano, Antonia Amelina, Beatrice Biferali, Alberto Macone, Chiara Mozzetta, Michele Maria Bianchi, Mattia Mori, Bruno Botta, Elah Pick, Rodolfo Negri & Teresa Rinaldi
Pages: 129-138
Published online: 07 Nov 2019
AbstractforStatins interfere with the attachment of S. cerevisiae mtDNA to the inner mitochondrial membrane | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 1822 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Synthesis, biological evaluation, and molecular modelling of new naphthalene-chalcone derivatives as potential anticancer agents on MCF-7 breast cancer cells by targeting tubulin colchicine binding site
Guangcheng Wang, Wenjing Liu, Zipeng Gong, Yong Huang, Yongjun Li & Zhiyun Peng
Pages: 139-144
Published online: 14 Nov 2019
AbstractforSynthesis, biological evaluation, and molecular modelling of new naphthalene-chalcone derivatives as potential anticancer agents on MCF-7 breast cancer cells by targeting tubulin colchicine binding site | Full Text | References | PDF (1 MB) | EPUB | Supplemental
  • 5012 Views
  • 52 CrossRef citations
  • 0Altmetric
Open Access
Article
Inhibition of SARS-CoV 3CL protease by flavonoids
Seri Jo, Suwon Kim, Dong Hae Shin & Mi-Sun Kim
Pages: 145-151
Published online: 14 Nov 2019
AbstractforInhibition of SARS-CoV 3CL protease by flavonoids | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 39184 Views
  • 452 CrossRef citations
  • 0Altmetric
Open Access
Article
Design and synthesis of tricyclic terpenoid derivatives as novel PTP1B inhibitors with improved pharmacological property and in vivo antihyperglycaemic efficacy
Lingling Yang, Feng Chen, Cheng Gao, Jiabao Chen, Junyan Li, Siyan Liu, Yuanyuan Zhang, Zhouyu Wang & Shan Qian
Pages: 152-164
Published online: 19 Nov 2019
AbstractforDesign and synthesis of tricyclic terpenoid derivatives as novel PTP1B inhibitors with improved pharmacological property and in vivo antihyperglycaemic efficacy | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 3229 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli & Claudiu T. Supuran
Pages: 165-171
Published online: 22 Nov 2019
AbstractforFurther validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 976 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Identifying novel sphingosine kinase 1 inhibitors as therapeutics against breast cancer
Faez Iqbal Khan, Dakun Lai, Razique Anwer, Iffat Azim & Mohd Kalim Ahmad Khan
Pages: 172-186
Published online: 22 Nov 2019
AbstractforIdentifying novel sphingosine kinase 1 inhibitors as therapeutics against breast cancer | Full Text | References | PDF (2.7 MB) | EPUB
  • 3287 Views
  • 25 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of talmapimod analogues as polypharmacological anti-inflammatory agents
Wandong Liu, Caiyun Hou, Jiaming Li, Xiaodong Ma, Yanchun Zhang, Mengqi Hu & Yuanzheng Huang
Pages: 187-198
Published online: 22 Nov 2019
AbstractforDiscovery of talmapimod analogues as polypharmacological anti-inflammatory agents | Full Text | References | PDF (1.7 MB)
  • 1600 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Towards discovery of new leishmanicidal scaffolds able to inhibit Leishmania GSK-3
Paula Martínez de Iturrate, Victor Sebastián-Pérez, Montserrat Nácher-Vázquez, Catherine S. Tremper, Despina Smirlis, Julio Martín, Ana Martínez, Nuria E. Campillo, Luis Rivas & Carmen Gil
Pages: 199-210
Published online: 22 Nov 2019
AbstractforTowards discovery of new leishmanicidal scaffolds able to inhibit Leishmania GSK-3 | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 2260 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel tacrine–benzofuran hybrids as potential multi-target drug candidates for the treatment of Alzheimer’s Disease
Gaia Fancellu, Karam Chand, Daniel Tomás, Elisabetta Orlandini, Luca Piemontese, Diana F. Silva, Sandra M. Cardoso, Sílvia Chaves & M. Amélia Santos
Pages: 211-226
Published online: 25 Nov 2019
AbstractforNovel tacrine–benzofuran hybrids as potential multi-target drug candidates for the treatment of Alzheimer’s Disease | Full Text | References | PDF (2.8 MB)
  • 3574 Views
  • 37 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors
Dong Jin Hong, Seung Hyun Jung, Jisook Kim, Danbee Jung, Young Gil Ahn, Kwee Hyun Suh & Kyung Hoon Min
Pages: 227-234
Published online: 22 Nov 2019
AbstractforSynthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors | Full Text | References | PDF (1 MB) | EPUB
  • 2284 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Identification of novel CDK2 inhibitors by a multistage virtual screening method based on SVM, pharmacophore and docking model
Jing-Wei Liang, Ming-Yang Wang, Shan Wang, Shi-Long Li, Wan-Qiu Li & Fan-Hao Meng
Pages: 235-244
Published online: 25 Nov 2019
AbstractforIdentification of novel CDK2 inhibitors by a multistage virtual screening method based on SVM, pharmacophore and docking model | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 3929 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Aryl derivatives of 3H-1,2-benzoxathiepine 2,2-dioxide as carbonic anhydrase inhibitors
Aleksandrs Pustenko, Alessio Nocentini, Anastasija Balašova, Ahmed Alafeefy, Mikhail Krasavin, Raivis Žalubovskis & Claudiu T. Supuran
Pages: 245-254
Published online: 02 Dec 2019
AbstractforAryl derivatives of 3H-1,2-benzoxathiepine 2,2-dioxide as carbonic anhydrase inhibitors | Full Text | References | PDF (2.5 MB) | EPUB
  • 1337 Views
  • 16 CrossRef citations
  • 0Altmetric
Open Access
Carbonic anhydrase IX as a novel candidate in liquid biopsy
Ozen Ozensoy Guler, Claudiu. T. Supuran & Clemente Capasso
Pages: 255-260
Published online: 02 Dec 2019
AbstractforCarbonic anhydrase IX as a novel candidate in liquid biopsy | Full Text | References | PDF (858.3 KB) | EPUB
  • 2619 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Evaluation of the paraoxonase-1 kinetic parameters of the lactonase activity by nonlinear fit of progress curves
Marko Goličnik & Aljoša Bavec
Pages: 261-264
Published online: 02 Dec 2019
AbstractforEvaluation of the paraoxonase-1 kinetic parameters of the lactonase activity by nonlinear fit of progress curves | Full Text | References | PDF (536.5 KB) | EPUB
  • 1178 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Benzothiazole derivatives as anticancer agents
Ali Irfan, Fozia Batool, Syeda Andleeb Zahra Naqvi, Amjad Islam, Sameh M. Osman, Alessio Nocentini, Siham A. Alissa & Claudiu T. Supuran
Pages: 265-279
Published online: 02 Dec 2019
AbstractforBenzothiazole derivatives as anticancer agents | Full Text | References | PDF (3.4 MB) | EPUB
  • 11553 Views
  • 125 CrossRef citations
  • 0Altmetric
Open Access
Article
Plasmatic exosomes from prostate cancer patients show increased carbonic anhydrase IX expression and activity and low pH
Mariantonia Logozzi, Davide Mizzoni, Clemente Capasso, Sonia Del Prete, Rossella Di Raimo, Mario Falchi, Daniela F. Angelini, Alessandro Sciarra, Martina Maggi, Claudiu T. Supuran & Stefano Fais
Pages: 280-288
Published online: 02 Dec 2019
AbstractforPlasmatic exosomes from prostate cancer patients show increased carbonic anhydrase IX expression and activity and low pH | Full Text | References | PDF (1.2 MB) | EPUB
  • 2768 Views
  • 43 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors
Yazgı Dizdaroglu, Canan Albay, Tayfun Arslan, Abdulilah Ece, Emir A. Turkoglu, Asiye Efe, Murat Senturk, Claudiu T. Supuran & Deniz Ekinci
Pages: 289-297
Published online: 04 Dec 2019
AbstractforDesign, synthesis and molecular modelling studies of some pyrazole derivatives as carbonic anhydrase inhibitors | Full Text | References | PDF (1.4 MB)
  • 4266 Views
  • 34 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and in vitro biological evaluation
Mohamed A. Abdelrahman, Wagdy M. Eldehna, Alessio Nocentini, Hany S. Ibrahim, Hadia Almahli, Hatem A. Abdel-Aziz, Sahar M. Abou-Seri & Claudiu T. Supuran
Pages: 298-305
Published online: 06 Dec 2019
AbstractforNovel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and in vitro biological evaluation | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 1799 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Screening of benzenesulfonamide in combination with chemically diverse fragments against carbonic anhydrase by differential scanning fluorimetry
Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasiia Gryniukova, Petro Borysko, Andrea Angeli & Claudiu T. Supuran
Pages: 306-310
Published online: 04 Dec 2019
AbstractforScreening of benzenesulfonamide in combination with chemically diverse fragments against carbonic anhydrase by differential scanning fluorimetry | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 1845 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Reprofiling of pyrimidine-based DAPK1/CSF1R dual inhibitors: identification of 2,5-diamino-4-pyrimidinol derivatives as novel potential anticancer lead compounds
Ahmed K. Farag, Ahmed H. E. Hassan, Byung Sun Ahn, Ki Duk Park & Eun Joo Roh
Pages: 311-324
Published online: 06 Dec 2019
AbstractforReprofiling of pyrimidine-based DAPK1/CSF1R dual inhibitors: identification of 2,5-diamino-4-pyrimidinol derivatives as novel potential anticancer lead compounds | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 2939 Views
  • 23 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties
Sinan Bilginer, Baris Gonder, Halise Inci Gul, Ruya Kaya, Ilhami Gulcin, Baris Anil & Claudiu T. Supuran
Pages: 325-329
Published online: 09 Dec 2019
AbstractforNovel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties | Full Text | References | PDF (773.6 KB) | EPUB
  • 1624 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease
Jun Mo, Tingkai Chen, Hongyu Yang, Yan Guo, Qi Li, Yuting Qiao, Hongzhi Lin, Feng Feng, Wenyuan Liu, Yao Chen, Zongliang Liu & Haopeng Sun
Pages: 330-343
Published online: 20 Dec 2019
AbstractforDesign, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer’s disease | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 3612 Views
  • 18 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions
Yuan Zhang, Xin Meng, Haikang Tang, Minghui Cheng, Fujun Yang & Wenqing Xu
Pages: 344-353
Published online: 18 Dec 2019
AbstractforDesign, synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 2963 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety
Xianqing Deng & Mingxia Song
Pages: 354-364
Published online: 18 Dec 2019
AbstractforSynthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety | Full Text | References | PDF (1.2 MB) | EPUB
  • 2364 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Development of a cheminformatics platform for selectivity analyses of carbonic anhydrase inhibitors
Giulio Poli, Salvatore Galati, Adriano Martinelli, Claudiu T. Supuran & Tiziano Tuccinardi
Pages: 365-371
Published online: 19 Dec 2019
AbstractforDevelopment of a cheminformatics platform for selectivity analyses of carbonic anhydrase inhibitors | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1392 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3
Youri Oh, Miyoung Jang, Hyunwook Cho, Songyi Yang, Daseul Im, Hyungwoo Moon & Jung-Mi Hah
Pages: 372-376
Published online: 19 Dec 2019
AbstractforDiscovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3 | Full Text | References | PDF (1.3 MB) | EPUB
  • 1476 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Inhibition survey with phenolic compounds against the δ- and η-class carbonic anhydrases from the marine diatom thalassiosira weissflogii and protozoan Plasmodium falciparum
Siham A. Alissa, Hanan A. Alghulikah, Zeid A. ALOthman, Sameh M. Osman, Sonia Del Prete, Clemente Capasso, Alessio Nocentini & Claudiu T. Supuran
Pages: 377-382
Published online: 19 Dec 2019
AbstractforInhibition survey with phenolic compounds against the δ- and η-class carbonic anhydrases from the marine diatom thalassiosira weissflogii and protozoan Plasmodium falciparum | Full Text | References | PDF (1,005.9 KB)
  • 1254 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and biological evaluation of carbohydrate-based sulphonamide derivatives as topical antiglaucoma agents through selective inhibition of carbonic anhydrase II
Zhuang Hou, Chuanchao Li, Yichuang Liu, Miao Zhang, Yitong Wang, Zhanfang Fan, Chun Guo, Bin Lin & Yang Liu
Pages: 383-390
Published online: 22 Dec 2019
AbstractforDesign, synthesis and biological evaluation of carbohydrate-based sulphonamide derivatives as topical antiglaucoma agents through selective inhibition of carbonic anhydrase II | Full Text | References | PDF (1.5 MB) | Supplemental
  • 2084 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
A potentiated cooperation of carbonic anhydrase IX and histone deacetylase inhibitors against cancer
Jessica Ruzzolini, Anna Laurenzana, Elena Andreucci, Silvia Peppicelli, Francesca Bianchini, Fabrizio Carta, Claudiu T. Supuran, Maria Novella Romanelli, Chiara Nediani & Lido Calorini
Pages: 391-397
Published online: 22 Dec 2019
AbstractforA potentiated cooperation of carbonic anhydrase IX and histone deacetylase inhibitors against cancer | Full Text | References | PDF (1.4 MB) | EPUB
  • 2503 Views
  • 16 CrossRef citations
  • 0Altmetric
Open Access
Article
Biological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent
Fabrice Pagniez, Nicolas Lebouvier, Young Min Na, Isabelle Ourliac-Garnier, Carine Picot, Marc Le Borgne & Patrice Le Pape
Pages: 398-403
Published online: 03 Jan 2020
AbstractforBiological exploration of a novel 1,2,4-triazole-indole hybrid molecule as antifungal agent | Full Text | References | PDF (1.2 MB)
  • 2080 Views
  • 32 CrossRef citations
  • 0Altmetric
Open Access
Article
N-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation
Wei-Yi Li, Wei-Wei Ni, Ya-Xi Ye, Hai-Lian Fang, Xing-Ming Pan, Jie-Ling He, Tian-Li Zhou, Juan Yi, Shan-Shan Liu, Mi Zhou, Zhu-Ping Xiao & Hai-Liang Zhu
Pages: 404-413
Published online: 27 Dec 2019
AbstractforN-monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 2527 Views
  • 35 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Novel CDKs inhibitors for the treatment of solid tumour by simultaneously regulating the cell cycle and transcription control
Xin Wang, Kaiyuan Deng, Cheng Wang, Yao Li, Tianqi Wang, Zhi Huang, Yakun Ma, Peiqing Sun, Yi Shi, Shengyong Yang, Yan Fan & Rong Xiang
Pages: 414-423
Published online: 03 Jan 2020
AbstractforNovel CDKs inhibitors for the treatment of solid tumour by simultaneously regulating the cell cycle and transcription control | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 2712 Views
  • 16 CrossRef citations
  • 0Altmetric
Open Access
Article
Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile
Nabih Lolak, Mehmet Boga, Muhammed Tuneg, Gulcin Karakoc, Suleyman Akocak & Claudiu T. Supuran
Pages: 424-431
Published online: 03 Jan 2020
AbstractforSulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile | Full Text | References | PDF (1.6 MB)
  • 2408 Views
  • 23 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and antiprotozoal evaluation of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives
Jean Guillon, Anita Cohen, Clotilde Boudot, Alessandra Valle, Vittoria Milano, Rabindra Nath Das, Aurore Guédin, Stéphane Moreau, Luisa Ronga, Solène Savrimoutou, Maxime Demourgues, Elodie Reviriego, Sandra Rubio, Sandie Ferriez, Patrice Agnamey, Cécile Pauc, Serge Moukha, Pascale Dozolme, Sophie Da Nascimento, Pierre Laumaillé, Anne Bouchut, Nadine Azas, Jean-Louis Mergny, Catherine Mullié, Pascal Sonnet & Bertrand Courtioux
Pages: 432-459
Published online: 03 Jan 2020
AbstractforDesign, synthesis, and antiprotozoal evaluation of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 2446 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives
Ivana Šagud, Nikolina Maček Hrvat, Ana Grgičević, Tena Čadež, Josipa Hodak, Milena Dragojević, Kornelija Lasić, Zrinka Kovarik & Irena Škorić
Pages: 460-467
Published online: 03 Jan 2020
AbstractforDesign, synthesis and cholinesterase inhibitory properties of new oxazole benzylamine derivatives | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
  • 1859 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological evaluation of novel (E)-N'-benzylidene hydrazides as novel c-Met inhibitors through fragment based virtual screening
Jing-wei Liang, Shi-long Li, Shan Wang, Wan-qiu Li & Fan-hao Meng
Pages: 468-477
Published online: 06 Jan 2020
AbstractforSynthesis and biological evaluation of novel (E)-N'-benzylidene hydrazides as novel c-Met inhibitors through fragment based virtual screening | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1845 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, in vitro screening and molecular docking of isoquinolinium-5-carbaldoximes as acetylcholinesterase and butyrylcholinesterase reactivators
David Malinak, Rafael Dolezal, Vendula Hepnarova, Miroslava Hozova, Rudolf Andrys, Petr Bzonek, Veronika Racakova, Jan Korabecny, Lukas Gorecki, Eva Mezeiova, Miroslav Psotka, Daniel Jun, Kamil Kuca & Kamil Musilek
Pages: 478-488
Published online: 07 Jan 2020
AbstractforSynthesis, in vitro screening and molecular docking of isoquinolinium-5-carbaldoximes as acetylcholinesterase and butyrylcholinesterase reactivators | Full Text | References | PDF (2.6 MB) | EPUB
  • 1965 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and human carbonic anhydrase I, II, VA, and XII inhibition with novel amino acid–sulphonamide conjugates
Hasan Küçükbay, Nesrin Buğday, F. Zehra Küçükbay, Andrea Ageli, Gianluca Bartolucci & Claudiu T. Supuran
Pages: 489-497
Published online: 08 Jan 2020
AbstractforSynthesis and human carbonic anhydrase I, II, VA, and XII inhibition with novel amino acid–sulphonamide conjugates | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1382 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Development of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probes
Stane Pajk, Damijan Knez, Urban Košak, Maja Zorović, Xavier Brazzolotto, Nicolas Coquelle, Florian Nachon, Jacques-Philippe Colletier, Marko Živin, Jure Stojan & Stanislav Gobec
Pages: 498-505
Published online: 08 Jan 2020
AbstractforDevelopment of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probes | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2884 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Sulfocoumarins as dual inhibitors of human carbonic anhydrase isoforms IX/XII and of human thioredoxin reductase
Mikhail Krasavin, Raivis Žalubovskis, Aiga Grandāne, Ilona Domračeva, Petr Zhmurov & Claudiu T. Supuran
Pages: 506-510
Published online: 13 Jan 2020
AbstractforSulfocoumarins as dual inhibitors of human carbonic anhydrase isoforms IX/XII and of human thioredoxin reductase | Full Text | References | PDF (813.1 KB) | EPUB
  • 1660 Views
  • 30 CrossRef citations
  • 0Altmetric
Open Access
Article
Deciphering the enzymatic target of a new family of antischistosomal agents bearing a quinazoline scaffold using complementary computational tools
Victor Sebastian-Perez, Alfonso García-Rubia, Sayed H. Seif el-Din, Abdel-Nasser A. Sabra, Naglaa M. El-Lakkany, Samia William, Tom L. Blundell, Louis Maes, Ana Martinez, Nuria E. Campillo, Sanaa S. Botros & Carmen Gil
Pages: 511-523
Published online: 15 Jan 2020
AbstractforDeciphering the enzymatic target of a new family of antischistosomal agents bearing a quinazoline scaffold using complementary computational tools | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 1474 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Effect of 6-Benzoyl-benzothiazol-2-one scaffold on the pharmacological profile of α-alkoxyphenylpropionic acid derived PPAR agonists
Aurélie Hurtevent, Morgan Le Naour, Veronique Leclerc, Pascal Carato, Patricia Melnyk, Nathalie Hennuyer, Bart Staels, Monique Beucher-Gaudin, Daniel-Henri Caignard, Catherine Dacquet & Nicolas Lebegue
Pages: 524-538
Published online: 15 Jan 2020
AbstractforEffect of 6-Benzoyl-benzothiazol-2-one scaffold on the pharmacological profile of α-alkoxyphenylpropionic acid derived PPAR agonists | Full Text | References | PDF (1.9 MB) | EPUB
  • 1656 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Coumarins from Magydaris pastinacea as inhibitors of the tumour-associated carbonic anhydrases IX and XII: isolation, biological studies and in silico evaluation
Benedetta Fois, Simona Distinto, Rita Meleddu, Serenella Deplano, Elias Maccioni, Costantino Floris, Antonella Rosa, Mariella Nieddu, Pierluigi Caboni, Claudia Sissi, Andrea Angeli, Claudiu T. Supuran & Filippo Cottiglia
Pages: 539-548
Published online: 17 Jan 2020
AbstractforCoumarins from Magydaris pastinacea as inhibitors of the tumour-associated carbonic anhydrases IX and XII: isolation, biological studies and in silico evaluation | Full Text | References | PDF (2.4 MB)
  • 2011 Views
  • 21 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
A class of carbonic anhydrase IX/XII – selective carboxylate inhibitors
Rakia Abd Alhameed, Emanuela Berrino, Zainab Almarhoon, Ayman El-Faham & Claudiu T. Supuran
Pages: 549-554
Published online: 22 Jan 2020
AbstractforA class of carbonic anhydrase IX/XII – selective carboxylate inhibitors | Full Text | References | PDF (860.4 KB) | EPUB
  • 1812 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Design, synthesis and in vitro biological evaluation of quinazolinone derivatives as EGFR inhibitors for antitumor treatment
Yi Le, Yiyuan Gan, Yihong Fu, Jiamin Liu, Wen Li, Xue Zou, Zhixu Zhou, Zhenchao Wang, Guiping Ouyang & Longjia Yan
Pages: 555-564
Published online: 22 Jan 2020
AbstractforDesign, synthesis and in vitro biological evaluation of quinazolinone derivatives as EGFR inhibitors for antitumor treatment | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 3466 Views
  • 47 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Design, synthesis and α-glucosidase inhibition study of novel embelin derivatives
Xiaole Chen, Min Gao, Rongchao Jian, Weiqian David Hong, Xiaowen Tang, Yuling Li, Denggao Zhao, Kun Zhang, Wenhua Chen, Xi Zheng, Zhaojun Sheng & Panpan Wu
Pages: 565-573
Published online: 22 Jan 2020
AbstractforDesign, synthesis and α-glucosidase inhibition study of novel embelin derivatives | Full Text | References | PDF (2.1 MB) | EPUB
  • 3153 Views
  • 19 CrossRef citations
  • 0Altmetric
Open Access
Selective inhibitors for JNK signalling: a potential targeted therapy in cancer
Qinghua Wu, Wenda Wu, Vesna Jacevic, Tanos C. C. Franca, Xu Wang & Kamil Kuca
Pages: 574-583
Published online: 29 Jan 2020
AbstractforSelective inhibitors for JNK signalling: a potential targeted therapy in cancer | Full Text | References | PDF (1.4 MB) | EPUB
  • 9238 Views
  • 76 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
C-2 phenyl replacements to obtain potent quinoline-based Staphylococcus aureus NorA inhibitors
Tommaso Felicetti, Gianmarco Mangiaterra, Rolando Cannalire, Nicholas Cedraro, Donatella Pietrella, Andrea Astolfi, Serena Massari, Oriana Tabarrini, Giuseppe Manfroni, Maria Letizia Barreca, Violetta Cecchetti, Francesca Biavasco & Stefano Sabatini
Pages: 584-597
Published online: 29 Jan 2020
AbstractforC-2 phenyl replacements to obtain potent quinoline-based Staphylococcus aureus NorA inhibitors | Full Text | References | PDF (2.8 MB) | EPUB
  • 5238 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Article
Exploring structure-activity relationship of S-substituted 2-mercaptoquinazolin-4(3H)-one including 4-ethylbenzenesulfonamides as human carbonic anhydrase inhibitors
Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Hany E. A. Ahmed, Sivia Bua, Alessio Nocentini, Nawaf A. AlSaif, Ahmad J. Obaidullah, Mohamed M. Hefnawy & Claudiu T. Supuran
Pages: 598-609
Published online: 02 Feb 2020
AbstractforExploring structure-activity relationship of S-substituted 2-mercaptoquinazolin-4(3H)-one including 4-ethylbenzenesulfonamides as human carbonic anhydrase inhibitors | Full Text | References | PDF (2.6 MB) | EPUB
  • 1624 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, anti-inflammatory, cytotoxic, and COX-1/2 inhibitory activities of cyclic imides bearing 3-benzenesulfonamide, oxime, and β-phenylalanine scaffolds: a molecular docking study
Alaa A.-M. Abdel-Aziz, Adel S. El-Azab, Nawaf A. AlSaif, Mohammed M. Alanazi, Manal A. El-Gendy, Ahmad J. Obaidullah, Hamad M. Alkahtani, Abdulrahman A. Almehizia & Ibrahim A. Al-Suwaidan
Pages: 610-621
Published online: 03 Feb 2020
AbstractforSynthesis, anti-inflammatory, cytotoxic, and COX-1/2 inhibitory activities of cyclic imides bearing 3-benzenesulfonamide, oxime, and β-phenylalanine scaffolds: a molecular docking study | Full Text | References | PDF (1.7 MB)
  • 2334 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation
Jeremie Brichet, Rodrigo Arancibia, Emanuela Berrino & Claudiu T. Supuran
Pages: 622-628
Published online: 10 Feb 2020
AbstractforBioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation | Full Text | References | PDF (938 KB) | Supplemental
  • 1193 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
Aspartic peptidase of Phialophora verrucosa as target of HIV peptidase inhibitors: blockage of its enzymatic activity and interference with fungal growth and macrophage interaction
Marcela Q. Granato, Ingrid S. Sousa, Thabatta L. S. A. Rosa, Diego S. Gonçalves, Sergio H. Seabra, Daniela S. Alviano, Maria C. V. Pessolani, André L. S. Santos & Lucimar F. Kneipp
Pages: 629-638
Published online: 10 Feb 2020
AbstractforAspartic peptidase of Phialophora verrucosa as target of HIV peptidase inhibitors: blockage of its enzymatic activity and interference with fungal growth and macrophage interaction | Full Text | References | PDF (1.6 MB) | EPUB
  • 1166 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of small molecule inhibitors of Leishmania braziliensis Hsp90 chaperone
Fernanda A. H. Batista, Sérgio L. Ramos Jr, Giusy Tassone, Andrei Leitão, Carlos A. Montanari, Maurizio Botta, Mattia Mori & Júlio C. Borges
Pages: 639-649
Published online: 12 Feb 2020
AbstractforDiscovery of small molecule inhibitors of Leishmania braziliensis Hsp90 chaperone | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 2306 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
7-Acylamino-3H-1,2-benzoxathiepine 2,2-dioxides as new isoform-selective carbonic anhydrase IX and XII inhibitors
Aleksandrs Pustenko, Alessio Nocentini, Anastasija Balašova, Mikhail Krasavin, Raivis Žalubovskis & Claudiu T. Supuran
Pages: 650-656
Published online: 21 Feb 2020
Abstractfor7-Acylamino-3H-1,2-benzoxathiepine 2,2-dioxides as new isoform-selective carbonic anhydrase IX and XII inhibitors | Full Text | References | PDF (1.4 MB)
  • 1125 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Article
In vivo antiaging effects of alkaline water supplementation
Mariantonia Logozzi, Davide Mizzoni, Rossella Di Raimo, Mauro Andreotti, Daniele Macchia, Massimo Spada & Stefano Fais
Pages: 657-664
Published online: 27 Feb 2020
AbstractforIn vivo antiaging effects of alkaline water supplementation | Full Text | References | PDF (1.1 MB) | EPUB
  • 7566 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Combining carbonic anhydrase and thioredoxin reductase inhibitory motifs within a single molecule dramatically increases its cytotoxicity
Mikhail Krasavin, Tatiana Sharonova, Vladimir Sharoyko, Daniil Zhukovsky, Stanislav Kalinin, Raivis Žalubovskis, Tatiana Tennikova & Claudiu T. Supuran
Pages: 665-671
Published online: 05 Mar 2020
AbstractforCombining carbonic anhydrase and thioredoxin reductase inhibitory motifs within a single molecule dramatically increases its cytotoxicity | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1099 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access
Article
Examination of sulfonamide-based inhibitors of MMP3 using the conditioned media of invasive glioma cells
Alisha T. Poole, Christopher A. Sitko, Caitlin Le, Christian C. Naus, Bryan M. Hill, Eric A. C. Bushnell & Vincent C. Chen
Pages: 672-681
Published online: 11 Mar 2020
AbstractforExamination of sulfonamide-based inhibitors of MMP3 using the conditioned media of invasive glioma cells | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1463 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Design, synthesis and antifungal activity of threoninamide carbamate derivatives via pharmacophore model
Xiu-Jiang Du, Xing-Jie Peng, Rui-Qi Zhao, Wei-Guang Zhao, Wei-Li Dong & Xing-Hai Liu
Pages: 682-691
Published online: 09 Mar 2020
AbstractforDesign, synthesis and antifungal activity of threoninamide carbamate derivatives via pharmacophore model | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 2127 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity
M. Ali, Assem Barakat, Ayman El-Faham, Hessa H. Al-Rasheed, Kholoud Dahlous, Abdullah Mohammed Al-Majid, Anamika Sharma, Sammer Yousuf, Mehar Sanam, Zaheer Ul-Haq, M. Iqbal Choudhary, Beatriz G. de la Torre & Fernando Albericio
Pages: 692-701
Published online: 11 Mar 2020
AbstractforSynthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 2267 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors
Myoung-Soon Park, Hyun-Ju Park, Young Jae An, Joon Hun Choi, Geunyoung Cha, Hwa Jeong Lee, So-Jung Park, Purushottam M. Dewang & Dae-Kee Kim
Pages: 702-712
Published online: 12 Mar 2020
AbstractforSynthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors | Full Text | References | PDF (1.5 MB) | EPUB
  • 1719 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of novel ATAD2 bromodomain inhibitors that trigger apoptosis and autophagy in breast cells by structure-based virtual screening
Dahong Yao, Jin Zhang, Jinhui Wang, Dabo Pan & Zhendan He
Pages: 713-725
Published online: 16 Mar 2020
AbstractforDiscovery of novel ATAD2 bromodomain inhibitors that trigger apoptosis and autophagy in breast cells by structure-based virtual screening | Full Text | References | PDF (4.1 MB) | EPUB
  • 3139 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Histidine residues at the copper-binding site in human tyrosinase are essential for its catalytic activities
Hyangsoon Noh, Sung Jun Lee, Hyun-Joo Jo, Hye Won Choi, Sungguan Hong & Kwang-Hoon Kong
Pages: 726-732
Published online: 17 Mar 2020
AbstractforHistidine residues at the copper-binding site in human tyrosinase are essential for its catalytic activities | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 2816 Views
  • 25 CrossRef citations
  • 0Altmetric
Open Access
Article
S-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors
Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Silvia Bua, Alessio Nocentini, Nawaf A. AlSaif, Mohammed M. Alanazi, Manal A. El-Gendy, Hany E. A. Ahmed & Claudiu T. Supuran
Pages: 733-743
Published online: 19 Mar 2020
AbstractforS-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1588 Views
  • 17 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, antitumor activity, and molecular docking study of 2-cyclopentyloxyanisole derivatives: mechanistic study of enzyme inhibition
Walaa M. El-Husseiny, Magda A.-A. El-Sayed, Adel S. El-Azab, Nawaf A. AlSaif, Mohammed M. Alanazi & Alaa A.-M. Abdel-Aziz
Pages: 744-758
Published online: 18 Mar 2020
AbstractforSynthesis, antitumor activity, and molecular docking study of 2-cyclopentyloxyanisole derivatives: mechanistic study of enzyme inhibition | Full Text | References | PDF (2.1 MB)
  • 2210 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways
Runwei Jiao, Fanxing Xu, Xiaofang Huang, Haonan Li, Weiwei Liu, Hao Cao, Linghe Zang, Zhanlin Li, Huiming Hua & Dahong Li
Pages: 759-772
Published online: 18 Mar 2020
AbstractforAntiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1589 Views
  • 18 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Design, synthesis and anticancer activity of naphthoquinone derivatives
Xiao-bao Shen, Yang Wang, Xuan-zhen Han, Liang-quan Sheng, Fu-fang Wu & Xinhua Liu
Pages: 773-785
Published online: 23 Mar 2020
AbstractforDesign, synthesis and anticancer activity of naphthoquinone derivatives | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 2259 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Article
Unveiling the interaction profile of rosmarinic acid and its bioactive substructures with serum albumin
Christina Papaemmanouil, Maria V. Chatziathanasiadou, Christos Chatzigiannis, Eleni Chontzopoulou, Thomas Mavromoustakos, Simona Golic Grdadolnik & Andreas G. Tzakos
Pages: 786-804
Published online: 23 Mar 2020
AbstractforUnveiling the interaction profile of rosmarinic acid and its bioactive substructures with serum albumin | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
  • 1861 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents
Jie Yang, Yinling Yun, Yuhang Miao, Jie Sun & Xiaojing Wang
Pages: 805-814
Published online: 18 Mar 2020
AbstractforSynthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer’s disease agents | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1683 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Exploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen
Alessandro Deplano, Jessica Karlsson, Mona Svensson, Federica Moraca, Bruno Catalanotti, Christopher J. Fowler & Valentina Onnis
Pages: 815-823
Published online: 23 Mar 2020
AbstractforExploring the fatty acid amide hydrolase and cyclooxygenase inhibitory properties of novel amide derivatives of ibuprofen | Full Text | References | PDF (2.1 MB) | EPUB
  • 1603 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Activation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids
Andrea Angeli, Sonia Del Prete, Cynthia Ghobril, Julien Hitce, Cécile Clavaud, Xavier Marrat, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 824-830
Published online: 27 Mar 2020
AbstractforActivation studies of the β-carbonic anhydrases from Malassezia restricta with amines and amino acids | Full Text | References | PDF (1.1 MB)
  • 954 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Rapid Communication
Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity
Sara T. Al-Rashood, Ahmed R. Hamed, Ghada S. Hassan, Hamad M. Alkahtani, Abdulrahman A. Almehizia, Amal Alharbi, Mohammad M. Al-Sanea & Wagdy M. Eldehna
Pages: 831-839
Published online: 25 Mar 2020
AbstractforAntitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity | Full Text | References | PDF (1.4 MB)
  • 2950 Views
  • 56 CrossRef citations
  • 0Altmetric
Open Access
Intra-site differential inhibition of multi-specific enzymes
Mario Cappiello, Francesco Balestri, Roberta Moschini, Umberto Mura & Antonella Del-Corso
Pages: 840-846
Published online: 25 Mar 2020
AbstractforIntra-site differential inhibition of multi-specific enzymes | Full Text | References | PDF (1 MB)
  • 1258 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors
Sahar A. Ali, Samir Mohamed Awad, Ahmed Mohammed Said, Shahenda Mahgoub, Heba Taha & Naglaa Mohamed Ahmed
Pages: 847-863
Published online: 27 Mar 2020
AbstractforDesign, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors | Full Text | References | PDF (2.6 MB) | EPUB
  • 3261 Views
  • 43 CrossRef citations
  • 0Altmetric
Open Access
Article
2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors
Phoebe F. Lamie & John N. Philoppes
Pages: 864-879
Published online: 25 Mar 2020
Abstractfor2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 2067 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and biological evaluation of (3/4-(pyrimidin-2-ylamino)benzoyl)-based hydrazine-1-carboxamide/carbothioamide derivatives as novel RXRα antagonists
Jingbo Qin, Jie Liu, Chunxiao Wu, Jianwen Xu, Bowen Tang, Kaiqiang Guo, Xiaohui Chen, Weihao Liu, Tong Wu, Hu Zhou, Meijuan Fang & Zhen Wu
Pages: 880-896
Published online: 30 Mar 2020
AbstractforSynthesis and biological evaluation of (3/4-(pyrimidin-2-ylamino)benzoyl)-based hydrazine-1-carboxamide/carbothioamide derivatives as novel RXRα antagonists | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1808 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Article
Strong inhibitory activities and action modes of lipopeptides on lipase
Mei-chun Chen, Tian-tian Liu, Jie-ping Wang, Yan-ping Chen, Qing-xi Chen, Yu-jing Zhu & Bo Liu
Pages: 897-905
Published online: 27 Mar 2020
AbstractforStrong inhibitory activities and action modes of lipopeptides on lipase | Full Text | References | PDF (1.9 MB) | EPUB
  • 1722 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75
Da-Wei Zhang, Hao-Li Yan, Xiao-Shuang Xu, Lei Xu, Zhi-Hui Yin, Shan Chang & Heng Luo
Pages: 906-912
Published online: 31 Mar 2020
AbstractforThe selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75 | Full Text | References | PDF (1.2 MB) | EPUB
  • 1950 Views
  • 20 CrossRef citations
  • 0Altmetric
Open Access
Article
Use of an immobilised thermostable α-CA (SspCA) for enhancing the metabolic efficiency of the freshwater green microalga Chlorella sorokiniana
Giovanna Salbitani, Sonia Del Prete, Francesco Bolinesi, Olga Mangoni, Viviana De Luca, Vincenzo Carginale, William A. Donald, Claudiu T. Supuran, Simona Carfagna & Clemente Capasso
Pages: 913-920
Published online: 30 Mar 2020
AbstractforUse of an immobilised thermostable α-CA (SspCA) for enhancing the metabolic efficiency of the freshwater green microalga Chlorella sorokiniana | Full Text | References | PDF (1.6 MB) | EPUB
  • 1581 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel sulindac derivatives: synthesis, characterisation, evaluation of antioxidant, analgesic, anti-inflammatory, ulcerogenic and COX-2 inhibition activity
Mashooq A. Bhat, Mohamed A. Al-Omar, Nawaf A. Alsaif, Abdulrahman A. Almehizia, Ahmed M. Naglah, Suhail Razak, Azmat Ali Khan & Naeem Mahmood Ashraf
Pages: 921-934
Published online: 02 Apr 2020
AbstractforNovel sulindac derivatives: synthesis, characterisation, evaluation of antioxidant, analgesic, anti-inflammatory, ulcerogenic and COX-2 inhibition activity | Full Text | References | PDF (2.2 MB) | EPUB
  • 1914 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity
Paul Le Baccon-Sollier, Yohan Malki, Morgane Maye, Lamiaa M. A. Ali, Laure Lichon, Pierre Cuq, Laure-Anaïs Vincent & Nicolas Masurier
Pages: 935-949
Published online: 05 Apr 2020
AbstractforImidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 1593 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
Mustafa Durgun, Cüneyt Türkeş, Mesut Işık, Yeliz Demir, Ali Saklı, Ali Kuru, Abdussamat Güzel, Şükrü Beydemir, Suleyman Akocak, Sameh M. Osman, Zeid AlOthman & Claudiu T. Supuran
Pages: 950-962
Published online: 05 Apr 2020
AbstractforSynthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases | Full Text | References | PDF (2.2 MB)
  • 4189 Views
  • 60 CrossRef citations
  • 0Altmetric
Open Access
Article
Lipidomic analysis of cancer cells cultivated at acidic pH reveals phospholipid fatty acids remodelling associated with transcriptional reprogramming
Lorena Urbanelli, Sandra Buratta, Mariantonia Logozzi, Nico Mitro, Krizia Sagini, Rossella Di Raimo, Donatella Caruso, Stefano Fais & Carla Emiliani
Pages: 963-973
Published online: 20 Apr 2020
AbstractforLipidomic analysis of cancer cells cultivated at acidic pH reveals phospholipid fatty acids remodelling associated with transcriptional reprogramming | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1821 Views
  • 16 CrossRef citations
  • 0Altmetric
Open Access
Article
6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers
Laura Braconi, Gianluca Bartolucci, Marialessandra Contino, Niccolò Chiaramonte, Roberta Giampietro, Dina Manetti, Maria Grazia Perrone, Maria Novella Romanelli, Nicola Antonio Colabufo, Chiara Riganti, Silvia Dei & Elisabetta Teodori
Pages: 974-992
Published online: 07 Apr 2020
Abstractfor6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers | Full Text | References | PDF (3.5 MB) | Supplemental
  • 1652 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy
Barbara Kaproń, Robert Czarnomysy, Mariusz Wysokiński, Rudolf Andrys, Kamil Musilek, Andrea Angeli, Claudiu T. Supuran & Tomasz Plech
Pages: 993-1002
Published online: 07 Apr 2020
Abstractfor1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy | Full Text | References | PDF (2 MB) | EPUB
  • 2122 Views
  • 26 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and carbonic anhydrase activating properties of a series of 2-amino-imidazolines structurally related to clonidine1
Niccolò Chiaramonte, Soumia Maach, Caterina Biliotti, Andrea Angeli, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Elisabetta Teodori, Claudiu T. Supuran & Maria Novella Romanelli
Pages: 1003-1010
Published online: 27 Apr 2020
AbstractforSynthesis and carbonic anhydrase activating properties of a series of 2-amino-imidazolines structurally related to clonidine1 | Full Text | References | PDF (1.4 MB) | EPUB
  • 1330 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
The antibiotic furagin and its derivatives are isoform-selective human carbonic anhydrase inhibitors
Aleksandrs Pustenko, Alessio Nocentini, Paola Gratteri, Alessandro Bonardi, Igor Vozny, Raivis Žalubovskis & Claudiu T. Supuran
Pages: 1011-1020
Published online: 16 Apr 2020
AbstractforThe antibiotic furagin and its derivatives are isoform-selective human carbonic anhydrase inhibitors | Full Text | References | PDF (2.9 MB) | Supplemental
  • 1927 Views
  • 26 CrossRef citations
  • 0Altmetric
Open Access
Article
Preparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety
Hasan Küçükbay, Zeynep Gönül, F. Zehra Küçükbay, Andrea Angeli, Gianluca Bartolucci & Claudiu T. Supuran
Pages: 1021-1026
Published online: 16 Apr 2020
AbstractforPreparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety | Full Text | References | PDF (1.7 MB)
  • 1025 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
An overview on natural farnesyltransferase inhibitors for efficient cancer therapy
Xiaohan Dai, Yingni Sun, Ting Zhang, Yongfei Ming & Gao Hongwei
Pages: 1027-1044
Published online: 20 Apr 2020
AbstractforAn overview on natural farnesyltransferase inhibitors for efficient cancer therapy | Full Text | References | PDF (1.8 MB) | EPUB
  • 5917 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Inhibition of African swine fever virus protease by myricetin and myricitrin
Seri Jo, Suwon Kim, Dong Hae Shin & Mi-Sun Kim
Pages: 1045-1049
Published online: 17 Apr 2020
AbstractforInhibition of African swine fever virus protease by myricetin and myricitrin | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 2522 Views
  • 21 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Antiproliferative benzothiazoles incorporating a trimethoxyphenyl scaffold as novel colchicine site tubulin polymerisation inhibitors
Dong-Jun Fu, Si-Meng Liu, Fu-Hao Li, Jia-Jia Yang & Jun Li
Pages: 1050-1059
Published online: 17 Apr 2020
AbstractforAntiproliferative benzothiazoles incorporating a trimethoxyphenyl scaffold as novel colchicine site tubulin polymerisation inhibitors | Full Text | References | PDF (1.9 MB) | EPUB
  • 1512 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Bacterial ι-carbonic anhydrase: a new active class of carbonic anhydrase identified in the genome of the Gram-negative bacterium Burkholderia territorii
Sonia Del Prete, Alessio Nocentini, Claudiu T. Supuran & Clemente Capasso
Pages: 1060-1068
Published online: 21 Apr 2020
AbstractforBacterial ι-carbonic anhydrase: a new active class of carbonic anhydrase identified in the genome of the Gram-negative bacterium Burkholderia territorii | Full Text | References | PDF (2.2 MB) | EPUB
  • 2895 Views
  • 74 CrossRef citations
  • 0Altmetric
Open Access
Article
Hybrid inhibitors of DNA and HDACs remarkably enhance cytotoxicity in leukaemia cells
Yoojin Song, Sun You Park, Zhexue Wu, Kwang-Hyeon Liu & Young Ho Seo
Pages: 1069-1079
Published online: 21 Apr 2020
AbstractforHybrid inhibitors of DNA and HDACs remarkably enhance cytotoxicity in leukaemia cells | Full Text | References | PDF (2.3 MB) | EPUB
  • 1481 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Chemical approaches for the enhancement of porphyrin skeleton-based photodynamic therapy
Yuyan Lin, Tao Zhou, Renren Bai & Yuanyuan Xie
Pages: 1080-1099
Published online: 24 Apr 2020
AbstractforChemical approaches for the enhancement of porphyrin skeleton-based photodynamic therapy | Full Text | References | PDF (2.6 MB) | EPUB
  • 5008 Views
  • 51 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells
Zeynep Özdemir, Semra Utku, Bijo Mathew, Simone Carradori, Giustino Orlando, Simonetta Di Simone, Mehmet Abdullah Alagöz, Azime Berna Özçelik, Mehtap Uysal & Claudio Ferrante
Pages: 1100-1109
Published online: 22 Apr 2020
AbstractforSynthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells | Full Text | References | PDF (1.8 MB) | EPUB
  • 1609 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Discovery of 5-methyl-N-(2-arylquinazolin-7-yl)isoxazole-4-carboxamide analogues as highly selective FLT3 inhibitors
Daseul Im, Hyungwoo Moon, Jinwoong Kim, Youri Oh, Miyoung Jang & Jung-Mi Hah
Pages: 1110-1115
Published online: 27 Apr 2020
AbstractforDiscovery of 5-methyl-N-(2-arylquinazolin-7-yl)isoxazole-4-carboxamide analogues as highly selective FLT3 inhibitors | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1326 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Design, synthesis and in vitro antiproliferative activity of new thiazolidinedione-1,3,4-oxadiazole hybrids as thymidylate synthase inhibitors
Zohor Mohammad Mahdi Alzhrani, Mohammad Mahboob Alam, Thikryat Neamatallah & Syed Nazreen
Pages: 1116-1123
Published online: 30 Apr 2020
AbstractforDesign, synthesis and in vitro antiproliferative activity of new thiazolidinedione-1,3,4-oxadiazole hybrids as thymidylate synthase inhibitors | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 2265 Views
  • 33 CrossRef citations
  • 0Altmetric
Open Access
Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat)
Sylvain Broussy, Hanna Laaroussi & Michel Vidal
Pages: 1124-1136
Published online: 05 May 2020
AbstractforBiochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat) | Full Text | References | PDF (1.6 MB) | EPUB
  • 3687 Views
  • 26 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Repurposing strategies on pyridazinone-based series by pharmacophore- and structure-driven screening
Giuseppe Floresta, Letizia Crocetti, Maria Paola Giovannoni, Pierfrancesco Biagini & Agostino Cilibrizzi
Pages: 1137-1144
Published online: 05 May 2020
AbstractforRepurposing strategies on pyridazinone-based series by pharmacophore- and structure-driven screening | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1469 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Natural compounds as inhibitors of transthyretin amyloidosis and neuroprotective agents: analysis of structural data for future drug design
Lidia Ciccone, Nicoló Tonali, Susanna Nencetti & Elisabetta Orlandini
Pages: 1145-1162
Published online: 18 May 2020
AbstractforNatural compounds as inhibitors of transthyretin amyloidosis and neuroprotective agents: analysis of structural data for future drug design | Full Text | References | PDF (3.8 MB) | EPUB
  • 4284 Views
  • 31 CrossRef citations
  • 0Altmetric
Open Access
Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade
Mateusz Daśko, Sebastian Demkowicz, Karol Biernacki, Olga Ciupak, Witold Kozak, Maciej Masłyk & Janusz Rachon
Pages: 1163-1184
Published online: 04 May 2020
AbstractforRecent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade | Full Text | References | PDF (5.6 MB) | EPUB
  • 1687 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
The Carbonic Anhydrase IX inhibitor SLC-0111 as emerging agent against the mesenchymal stem cell-derived pro-survival effects on melanoma cells
Silvia Peppicelli, Elena Andreucci, Jessica Ruzzolini, Francesca Bianchini, Chiara Nediani, Claudiu T. Supuran & Lido Calorini
Pages: 1185-1193
Published online: 12 May 2020
AbstractforThe Carbonic Anhydrase IX inhibitor SLC-0111 as emerging agent against the mesenchymal stem cell-derived pro-survival effects on melanoma cells | Full Text | References | PDF (1.9 MB) | Supplemental
  • 3754 Views
  • 21 CrossRef citations
  • 0Altmetric
Open Access
Article
Oxy-imino saccharidic derivatives as a new structural class of aldose reductase inhibitors endowed with anti-oxidant activity
Felicia D'Andrea, Stefania Sartini, Ilaria Piano, Matteo Franceschi, Luca Quattrini, Lorenzo Guazzelli, Lidia Ciccone, Elisabetta Orlandini, Claudia Gargini, Concettina La Motta & Susanna Nencetti
Pages: 1194-1205
Published online: 12 May 2020
AbstractforOxy-imino saccharidic derivatives as a new structural class of aldose reductase inhibitors endowed with anti-oxidant activity | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1247 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Carbonic anhydrase modulation of emotional memory. Implications for the treatment of cognitive disorders
Patrizio Blandina, Gustavo Provensi, Maria Beatrice Passani, Clemente Capasso & Claudiu T. Supuran
Pages: 1206-1214
Published online: 13 May 2020
AbstractforCarbonic anhydrase modulation of emotional memory. Implications for the treatment of cognitive disorders | Full Text | References | PDF (1.4 MB)
  • 2190 Views
  • 43 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis of calix[4]azacrown substituted sulphonamides with antioxidant, acetylcholinesterase, butyrylcholinesterase, tyrosinase and carbonic anhydrase inhibitory action
Mehmet Oguz, Erbay Kalay, Suleyman Akocak, Alessio Nocentini, Nebih Lolak, Mehmet Boga, Mustafa Yilmaz & Claudiu T. Supuran
Pages: 1215-1223
Published online: 13 May 2020
AbstractforSynthesis of calix[4]azacrown substituted sulphonamides with antioxidant, acetylcholinesterase, butyrylcholinesterase, tyrosinase and carbonic anhydrase inhibitory action | Full Text | References | PDF (1.4 MB)
  • 2002 Views
  • 19 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery and antibacterial study of potential PPK1 inhibitors against uropathogenic E. coli
Liang Peng, Liting Zeng, Hongwei Jin, Lixin Yang, Yi Xiao, Ziquan Lan, Zhanpeng Yu, Shi Ouyang, Liangren Zhang & Ning Sun
Pages: 1224-1232
Published online: 18 May 2020
AbstractforDiscovery and antibacterial study of potential PPK1 inhibitors against uropathogenic E. coli | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1872 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
A nanobody-derived mimotope against VEGF inhibits cancer angiogenesis
Elmira Karami, Jean-Marc Sabatier, Mahdi Behdani, Shiva Irani & Fatemeh Kazemi-Lomedasht
Pages: 1233-1239
Published online: 22 May 2020
AbstractforA nanobody-derived mimotope against VEGF inhibits cancer angiogenesis | Full Text | References | PDF (971.4 KB) | EPUB
  • 2627 Views
  • 19 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of secondary sulphonamides as IDO1 inhibitors with potent antitumour effects in vivo
Shushan Ge, Haiqing Zhong, Xuewei Ma, Yingbo Zheng, Yi Zou, Fang Wang, Yan Wang, Yue Hu, Yuezhen Li, Wen Liu, Wenjie Guo, Qiang Xu & Yisheng Lai
Pages: 1240-1257
Published online: 28 May 2020
AbstractforDiscovery of secondary sulphonamides as IDO1 inhibitors with potent antitumour effects in vivo | Full Text | References | PDF (6.1 MB) | EPUB
  • 2582 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Article
Prognostic value of CAIX expression in oral squamous cell carcinoma: a systematic review and meta-analysis
Alejandro I. Lorenzo-Pouso, Mercedes Gallas-Torreira, Mario Pérez-Sayáns, Cintia M. Chamorro-Petronacci, Oscar Alvarez-Calderon, Bahi Takkouche, Claudiu T. Supuran & Abel García-García
Pages: 1258-1266
Published online: 29 May 2020
AbstractforPrognostic value of CAIX expression in oral squamous cell carcinoma: a systematic review and meta-analysis | Full Text | References | PDF (1.8 MB) | EPUB
  • 1724 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Recent advances in modulators of circadian rhythms: an update and perspective
Shenzhen Huang, Xinwei Jiao, Dingli Lu, Xiaoting Pei, Di Qi & Zhijie Li
Pages: 1267-1286
Published online: 08 Jun 2020
AbstractforRecent advances in modulators of circadian rhythms: an update and perspective | Full Text | References | PDF (4.2 MB) | EPUB
  • 4424 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Screening of ninety herbal products of commercial interest as potential ingredients for phytocosmetics
Mariacaterina Lianza, Manuela Mandrone, Ilaria Chiocchio, Paola Tomasi, Lorenzo Marincich & Ferruccio Poli
Pages: 1287-1291
Published online: 09 Jun 2020
AbstractforScreening of ninety herbal products of commercial interest as potential ingredients for phytocosmetics | Full Text | References | PDF (533.3 KB) | EPUB
  • 2703 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Biochemical and structural characterisation of a protozoan beta-carbonic anhydrase from Trichomonas vaginalis
Linda J. Urbański, Anna Di Fiore, Latifeh Azizi, Vesa P. Hytönen, Marianne Kuuslahti, Martina Buonanno, Simona M. Monti, Andrea Angeli, Reza Zolfaghari Emameh, Claudiu T. Supuran, Giuseppina De Simone & Seppo Parkkila
Pages: 1292-1299
Published online: 09 Jun 2020
AbstractforBiochemical and structural characterisation of a protozoan beta-carbonic anhydrase from Trichomonas vaginalis | Full Text | References | PDF (1.9 MB) | EPUB
  • 1535 Views
  • 19 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel [(N-alkyl-3-indolylmethylene)hydrazono]oxindoles arrest cell cycle and induce cell apoptosis by inhibiting CDK2 and Bcl-2: synthesis, biological evaluation and in silico studies
Tarfah Al-Warhi, Mahmoud F. Abo-Ashour, Hadia Almahli, Ohoud J. Alotaibi, Mohammad M. Al-Sanea, Ghada H. Al-Ansary, Hanaa Y. Ahmed, Mahmoud M. Elaasser, Wagdy M. Eldehna & Hatem A. Abdel-Aziz
Pages: 1300-1309
Published online: 11 Jun 2020
AbstractforNovel [(N-alkyl-3-indolylmethylene)hydrazono]oxindoles arrest cell cycle and induce cell apoptosis by inhibiting CDK2 and Bcl-2: synthesis, biological evaluation and in silico studies | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2004 Views
  • 36 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety
Mingxia Song, Rui Yan, Yanhui Zhang, Dongfu Guo, Naiming Zhou & XianQing Deng
Pages: 1310-1321
Published online: 12 Jun 2020
AbstractforDesign, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety | Full Text | References | PDF (2.3 MB) | EPUB
  • 1429 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Advances in the discovery of exosome inhibitors in cancer
Huarui Zhang, Jun Lu, Jin Liu, Ge Zhang & Aiping Lu
Pages: 1322-1330
Published online: 16 Jun 2020
AbstractforAdvances in the discovery of exosome inhibitors in cancer | Full Text | References | PDF (1.9 MB) | EPUB
  • 9657 Views
  • 61 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and evaluation of a large library of nitroxoline derivatives as pancreatic cancer antiproliferative agents
Serena Veschi, Simone Carradori, Laura De Lellis, Rosalba Florio, Davide Brocco, Daniela Secci, Paolo Guglielmi, Mattia Spano, Anatoly P. Sobolev & Alessandro Cama
Pages: 1331-1344
Published online: 26 Jun 2020
AbstractforSynthesis and evaluation of a large library of nitroxoline derivatives as pancreatic cancer antiproliferative agents | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 1750 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania
Andrea Medeiros, Diego Benítez, Ricarda S. Korn, Vinicius C. Ferreira, Exequiel Barrera, Federico Carrión, Otto Pritsch, Sergio Pantano, Conrad Kunick, Camila I. de Oliveira, Oliver C. F. Orban & Marcelo A. Comini
Pages: 1345-1358
Published online: 26 Jun 2020
AbstractforMechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 1387 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
Onur Argan, Kübra Çıkrıkçı, Aybike Baltacı & Nahit Gencer
Pages: 1359-1362
Published online: 22 Jun 2020
AbstractforThe effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes | Full Text | References | PDF (853 KB) | EPUB
  • 1650 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Topoisomerases inhibition and DNA binding mode of daunomycin–oligoarginine conjugate
Valeria Visone, Ildikó Szabó, Giuseppe Perugino, Ferenc Hudecz, Zoltán Bánóczi & Anna Valenti
Pages: 1363-1371
Published online: 19 Jun 2020
AbstractforTopoisomerases inhibition and DNA binding mode of daunomycin–oligoarginine conjugate | Full Text | References | PDF (1.1 MB) | EPUB
  • 1265 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Article
Cinnamic acid derivatives: inhibitory activity against Escherichia coli β-glucuronidase and structure–activity relationships
Xing-Nuo Li, Lu-Xia Hua, Tao-Shun Zhou, Ke-Bo Wang, Yuan-Yuan Wu, Mahmoud Emam, Xiao-Ze Bao, Jun Chen & Bin Wei
Pages: 1372-1378
Published online: 22 Jun 2020
AbstractforCinnamic acid derivatives: inhibitory activity against Escherichia coli β-glucuronidase and structure–activity relationships | Full Text | References | PDF (1.5 MB) | EPUB
  • 1886 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
Activation studies of the β-carbonic anhydrases from Escherichia coli with amino acids and amines
Alessio Nocentini, Sonia Del Prete, Margaret D. Mastrolorenzo, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 1379-1386
Published online: 24 Jun 2020
AbstractforActivation studies of the β-carbonic anhydrases from Escherichia coli with amino acids and amines | Full Text | References | PDF (1.4 MB)
  • 855 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Design, synthesis, and in vitro evaluation of aza-peptide aldehydes and ketones as novel and selective protease inhibitors
Thomas S. Corrigan, Leilani M. Lotti Diaz, Sarah E. Border, Steven C. Ratigan, Kayla Q. Kasper, Daniel Sojka, Pavla Fajtova, Conor R. Caffrey, Guy S. Salvesen, Craig A. McElroy, Christopher M. Hadad & Özlem Doğan Ekici
Pages: 1387-1402
Published online: 07 Jul 2020
AbstractforDesign, synthesis, and in vitro evaluation of aza-peptide aldehydes and ketones as novel and selective protease inhibitors | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 4126 Views
  • 6 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells
Dong-Jun Fu, Si-Meng Liu, Jia-Jia Yang & Jun Li
Pages: 1403-1413
Published online: 26 Jun 2020
AbstractforNovel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1589 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
A study of Rose Bengal against a 2-keto-3-deoxy-d-manno-octulosonate cytidylyltransferase as an antibiotic candidate
Suwon Kim, Seri Jo, Mi-Sun Kim & Dong Hae Shin
Pages: 1414-1421
Published online: 26 Jun 2020
AbstractforA study of Rose Bengal against a 2-keto-3-deoxy-d-manno-octulosonate cytidylyltransferase as an antibiotic candidate | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1281 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, in vitro enzyme activity and molecular docking studies of new benzylamine-sulfonamide derivatives as selective MAO-B inhibitors
Begüm Nurpelin Sağlık, Derya Osmaniye, Ulviye Acar Çevik, Serkan Levent, Betül Kaya Çavuşoğlu, Özlem Atlı Eklioğlu, Yusuf Özkay, Ali Savaş Koparal & Zafer Asım Kaplancıklı
Pages: 1422-1432
Published online: 30 Jun 2020
AbstractforSynthesis, in vitro enzyme activity and molecular docking studies of new benzylamine-sulfonamide derivatives as selective MAO-B inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 2167 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
LC-QTOF-MS analysis of xanthone content in different parts of Garcinia mangostana and its influence on cholinesterase inhibition
Kooi Yeong Khaw, Chun Wie Chong & Vikneswaran Murugaiyah
Pages: 1433-1441
Published online: 01 Jul 2020
AbstractforLC-QTOF-MS analysis of xanthone content in different parts of Garcinia mangostana and its influence on cholinesterase inhibition | Full Text | References | PDF (1.6 MB) | EPUB
  • 1802 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, computational studies and assessment of in vitro inhibitory activity of umbelliferon-based compounds against tumour-associated carbonic anhydrase isoforms IX and XII
Francesca Mancuso, Laura De Luca, Andrea Angeli, Sonia Del Prete, Clemente Capasso, Claudiu T. Supuran & Rosaria Gitto
Pages: 1442-1449
Published online: 02 Jul 2020
AbstractforSynthesis, computational studies and assessment of in vitro inhibitory activity of umbelliferon-based compounds against tumour-associated carbonic anhydrase isoforms IX and XII | Full Text | References | PDF (1.9 MB) | EPUB
  • 1054 Views
  • 5 CrossRef citations
  • 0Altmetric
Open Access
Human carbonic anhydrases and post-translational modifications: a hidden world possibly affecting protein properties and functions
Anna Di Fiore, Claudiu T. Supuran, Andrea Scaloni & Giuseppina De Simone
Pages: 1450-1461
Published online: 10 Jul 2020
AbstractforHuman carbonic anhydrases and post-translational modifications: a hidden world possibly affecting protein properties and functions | Full Text | References | PDF (1.8 MB) | EPUB
  • 1881 Views
  • 19 CrossRef citations
  • 0Altmetric
Open Access
Coumarin carbonic anhydrase inhibitors from natural sources
Claudiu T. Supuran
Pages: 1462-1470
Published online: 11 Aug 2020
AbstractforCoumarin carbonic anhydrase inhibitors from natural sources | Full Text | References | PDF (1.4 MB)
  • 2792 Views
  • 51 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and structure-activity relationships of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives as 5-lipoxygenase inhibitors
Oludotun A. Phillips, Mira A. Bosso & Charles I. Ezeamuzie
Pages: 1471-1482
Published online: 08 Jul 2020
AbstractforSynthesis and structure-activity relationships of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives as 5-lipoxygenase inhibitors | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1271 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and evaluation of 2,4,5-trisubstitutedthiazoles as carbonic anhydrase-III inhibitors
Bilal A. Al-Jaidi, Pran Kishore Deb, Soha Taher Telfah, Abdel Naser Dakkah, Yazan A. Bataineh, Qutaiba Ahmed Al Khames Aga, Mohammad A. Al-dhoun, Ala’ Ali Ahmad Al-Subeihi, Haifa’a Marouf Odetallah, Sanaa K. Bardaweel, Raghuprasad Mailavaram, Katharigatta N. Venugopala & Anroop B. Nair
Pages: 1483-1490
Published online: 08 Jul 2020
AbstractforSynthesis and evaluation of 2,4,5-trisubstitutedthiazoles as carbonic anhydrase-III inhibitors | Full Text | References | PDF (1.8 MB) | EPUB
  • 1155 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel heterocyclic hybrids of pyrazole targeting dihydrofolate reductase: design, biological evaluation and insilico studies
Ismail M. M. Othman, Mohamed A. M. Gad-Elkareem, Abd El-Galil E. Amr, Mohamed A. Al-Omar, Eman S. Nossier & Elsayed A. Elsayed
Pages: 1491-1502
Published online: 16 Jul 2020
AbstractforNovel heterocyclic hybrids of pyrazole targeting dihydrofolate reductase: design, biological evaluation and insilico studies | Full Text | References | PDF (2.2 MB) | EPUB
  • 1936 Views
  • 28 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis and structure-activity relationships of cerebroside analogues as substrates of cerebroside sulphotransferase and discovery of a competitive inhibitor
Wenjin Li, Joren Guillaume, Younis Baqi, Isabell Wachsmann, Volkmar Gieselmann, Serge Van Calenbergh & Christa E. Müller
Pages: 1503-1512
Published online: 13 Jul 2020
AbstractforSynthesis and structure-activity relationships of cerebroside analogues as substrates of cerebroside sulphotransferase and discovery of a competitive inhibitor | Full Text | References | PDF (2.4 MB) | EPUB
  • 1294 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and evaluation of 1, 4-benzodioxan-substituted chalcones as selective and reversible inhibitors of human monoamine oxidase B
Zhuo Kong, Demeng Sun, Yanmei Jiang & Yun Hu
Pages: 1513-1523
Published online: 23 Jul 2020
AbstractforDesign, synthesis, and evaluation of 1, 4-benzodioxan-substituted chalcones as selective and reversible inhibitors of human monoamine oxidase B | Full Text | References | PDF (1.5 MB) | EPUB
  • 1194 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and biological evaluation of novel tetrahydrothieno [2,3-c]pyridine substitued benzoyl thiourea derivatives as PAK1 inhibitors in triple negative breast cancer
Dahong Yao, Jian Huang, Jinhui Wang, Zhendan He & Jin Zhang
Pages: 1524-1538
Published online: 04 Aug 2020
AbstractforDesign, synthesis and biological evaluation of novel tetrahydrothieno [2,3-c]pyridine substitued benzoyl thiourea derivatives as PAK1 inhibitors in triple negative breast cancer | Full Text | References | PDF (3.6 MB) | EPUB
  • 1255 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Flavonoids with inhibitory activity against SARS-CoV-2 3CLpro
Seri Jo, Suwon Kim, Dae Yong Kim, Mi-Sun Kim & Dong Hae Shin
Pages: 1539-1544
Published online: 04 Aug 2020
AbstractforFlavonoids with inhibitory activity against SARS-CoV-2 3CLpro | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
  • 7115 Views
  • 104 CrossRef citations
  • 0Altmetric
Open Access
Article
Escherichia coliγ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors
Sonia Del Prete, Silvia Bua, Claudiu T. Supuran & Clemente Capasso
Pages: 1545-1554
Published online: 04 Aug 2020
AbstractforEscherichia coliγ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors | Full Text | References | PDF (2.2 MB) | EPUB
  • 1388 Views
  • 25 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Inhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents
Mikhail Krasavin, Stanislav Kalinin, Tatiana Sharonova & Claudiu T. Supuran
Pages: 1555-1561
Published online: 04 Aug 2020
AbstractforInhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 1477 Views
  • 23 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Functionality study of chalcone-hydroxypyridinone hybrids as tyrosinase inhibitors and influence on anti-tyrosinase activity
L. Ravithej Singh, Yu-Lin Chen, Yuan-Yuan Xie, Wei Xia, Xing-Wen Gong, Robert C. Hider & Tao Zhou
Pages: 1562-1567
Published online: 04 Aug 2020
AbstractforFunctionality study of chalcone-hydroxypyridinone hybrids as tyrosinase inhibitors and influence on anti-tyrosinase activity | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 1519 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B
Ahmed Elkamhawy, Sora Paik, Hyeon Jeong Kim, Jong-Hyun Park, Ashwini M. Londhe, Kyeong Lee, Ae Nim Pae, Ki Duk Park & Eun Joo Roh
Pages: 1568-1580
Published online: 04 Aug 2020
AbstractforDiscovery of N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B | Full Text | References | PDF (2.3 MB) | EPUB
  • 1933 Views
  • 15 CrossRef citations
  • 0Altmetric
Open Access
Article
Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors
Monica-Cornelia Sardaru, Anda Mihaela Craciun, Cristina-Maria Al Matarneh, Isabela Andreea Sandu, Roxana Maria Amarandi, Lacramioara Popovici, Catalina Ionica Ciobanu, Dragos Peptanariu, Mariana Pinteala, Ionel I. Mangalagiu & Ramona Danac
Pages: 1581-1595
Published online: 04 Aug 2020
AbstractforCytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
  • 1565 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Design, synthesis and biological evaluation of edaravone derivatives bearing the N-benzyl pyridinium moiety as multifunctional anti-Alzheimer’s agents
Luke S. Zondagh, Sarel F. Malan & Jacques Joubert
Pages: 1596-1605
Published online: 11 Aug 2020
AbstractforDesign, synthesis and biological evaluation of edaravone derivatives bearing the N-benzyl pyridinium moiety as multifunctional anti-Alzheimer’s agents | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2674 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1)
Zhimin Zhang, Xinyue Chang, Chixiao Zhang, Shenxin Zeng, Meihao Liang, Zhen Ma, Zunyuan Wang, Wenhai Huang & Zhengrong Shen
Pages: 1606-1615
Published online: 11 Aug 2020
AbstractforIdentification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1) | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 3642 Views
  • 27 CrossRef citations
  • 0Altmetric
Open Access
Article
Discovery of 3,6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico insights
Ahmed Sabt, Wagdy M. Eldehna, Tarfah Al-Warhi, Ohoud J. Alotaibi, Mahmoud M. Elaasser, Howayda Suliman & Hatem A. Abdel-Aziz
Pages: 1616-1630
Published online: 11 Aug 2020
AbstractforDiscovery of 3,6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico insights | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 2251 Views
  • 36 CrossRef citations
  • 0Altmetric
Open Access
Article
Potential anti-neuroinflammatory NF-кB inhibitors based on 3,4-dihydronaphthalen-1(2H)-one derivatives
Yue Sun, Yan-Qiu Zhou, Yin-Kai Liu, Hong-Qin Zhang, Gui-Ge Hou, Qing-Guo Meng & Yun Hou
Pages: 1631-1640
Published online: 11 Aug 2020
AbstractforPotential anti-neuroinflammatory NF-кB inhibitors based on 3,4-dihydronaphthalen-1(2H)-one derivatives | Full Text | References | PDF (2.1 MB) | EPUB
  • 1728 Views
  • 34 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis and biological evaluation of a new thieno[2,3-d]pyrimidine-based urea derivative with potential antitumor activity against tamoxifen sensitive and resistant breast cancer cell lines
Marwa Sharaky, Marwa Kamel, Marwa A. Aziz, Mervat Omran, Monira M. Rageh, Khaled A. M. Abouzid & Samia A. Shouman
Pages: 1641-1656
Published online: 11 Aug 2020
AbstractforDesign, synthesis and biological evaluation of a new thieno[2,3-d]pyrimidine-based urea derivative with potential antitumor activity against tamoxifen sensitive and resistant breast cancer cell lines | Full Text | References | PDF (4.7 MB) | EPUB | Supplemental
  • 2419 Views
  • 13 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison
Ulviye Acar Çevik, Begüm Nurpelin Sağlık, Derya Osmaniye, Serkan Levent, Betül Kaya Çavuşoğlu, Abdullah Burak Karaduman, Özlem Atlı Eklioğlu, Yusuf Özkay & Zafer Asım Kaplancıklı
Pages: 1657-1673
Published online: 19 Aug 2020
AbstractforSynthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison | Full Text | References | PDF (4.9 MB) | EPUB | Supplemental
  • 2514 Views
  • 21 CrossRef citations
  • 0Altmetric
Open Access
Article
Efficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors
Loghman Firoozpour, Lixin Gao, Setareh Moghimi, Parvin Pasalar, Jamshid Davoodi, Ming-Wei Wang, Zahra Rezaei, Armin Dadgar, Hoda Yahyavi, Massoud Amanlou & Alireza Foroumadi
Pages: 1674-1684
Published online: 25 Aug 2020
AbstractforEfficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors | Full Text | References | PDF (1.5 MB) | EPUB
  • 1741 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
New classes of potent heparanase inhibitors from ligand-based virtual screening
Daniele Pala, Laura Scalvini, Gian Marco Elisi, Alessio Lodola, Marco Mor, Gilberto Spadoni, Fabiana F. Ferrara, Emiliano Pavoni, Giuseppe Roscilli, Ferdinando M. Milazzo, Gianfranco Battistuzzi, Silvia Rivara & Giuseppe Giannini
Pages: 1685-1696
Published online: 09 Sep 2020
AbstractforNew classes of potent heparanase inhibitors from ligand-based virtual screening | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
  • 1930 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
The intensification of anticancer activity of LFM-A13 by erythropoietin as a possible option for inhibition of breast cancer
Dariusz Rozkiewicz, Justyna Magdalena Hermanowicz, Anna Tankiewicz-Kwedlo, Beata Sieklucka, Krystyna Pawlak, Robert Czarnomysy, Krzysztof Bielawski, Arkadiusz Surazynski, Joanna Kalafut, Alicja Przybyszewska, Mariusz Koda, Katarzyna Jakubowska, Adolfo Rivero-Muller & Dariusz Pawlak
Pages: 1697-1711
Published online: 10 Sep 2020
AbstractforThe intensification of anticancer activity of LFM-A13 by erythropoietin as a possible option for inhibition of breast cancer | Full Text | References | PDF (3.8 MB) | EPUB
  • 1367 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies
Hanan S. Anbar, Mohammed I. El-Gamal, Hamadeh Tarazi, Bong S. Lee, Hong R. Jeon, Dow Kwon & Chang-Hyun Oh
Pages: 1712-1726
Published online: 23 Sep 2020
AbstractforImidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies | Full Text | References | PDF (3.2 MB) | EPUB
  • 1499 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Article
Rational design of small molecules able to inhibit α-synuclein amyloid aggregation for the treatment of Parkinson’s disease
Serena Vittorio, Ilenia Adornato, Rosaria Gitto, Samuel Peña-Díaz, Salvador Ventura & Laura De Luca
Pages: 1727-1735
Published online: 14 Sep 2020
AbstractforRational design of small molecules able to inhibit α-synuclein amyloid aggregation for the treatment of Parkinson’s disease | Full Text | References | PDF (3.1 MB) | EPUB
  • 2844 Views
  • 17 CrossRef citations
  • 0Altmetric
Open Access
Article
Thiazolidin-2-cyanamides derivatives as novel potent Escherichia coli β-glucuronidase inhibitors and their structure–inhibitory activity relationships
Tao-Shun Zhou, Bin Wei, Min He, Ya-Sheng Li, Ya-Kun Wang, Si-Jia Wang, Jian-Wei Chen, Hua-Wei Zhang, Zi-Ning Cui & Hong Wang
Pages: 1736-1742
Published online: 14 Sep 2020
AbstractforThiazolidin-2-cyanamides derivatives as novel potent Escherichia coli β-glucuronidase inhibitors and their structure–inhibitory activity relationships | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 1320 Views
  • 11 CrossRef citations
  • 0Altmetric
Open Access
Article
Quetiapine and novel PDE10A inhibitors potentiate the anti-BuChE activity of donepezil
Joanna Sikora, Maria Podsiedlik, Tadeusz Pietras, Marcin Kosmalski, Mikołaj Matłoka, Rafał Moszczyński-Petkowski, Maciej Wieczorek & Magdalena Markowicz-Piasecka
Pages: 1743-1750
Published online: 17 Sep 2020
AbstractforQuetiapine and novel PDE10A inhibitors potentiate the anti-BuChE activity of donepezil | Full Text | References | PDF (1.1 MB) | EPUB
  • 1327 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Novel temporin L antimicrobial peptides: promoting self-assembling by lipidic tags to tackle superbugs
Rosa Bellavita, Annarita Falanga, Elisabetta Buommino, Francesco Merlino, Bruno Casciaro, Floriana Cappiello, Maria Luisa Mangoni, Ettore Novellino, Maria Rosaria Catania, Rossella Paolillo, Paolo Grieco & Stefania Galdiero
Pages: 1751-1764
Published online: 22 Sep 2020
AbstractforNovel temporin L antimicrobial peptides: promoting self-assembling by lipidic tags to tackle superbugs | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1924 Views
  • 16 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Toxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases
Ashok Aspatwar, Emanuela Berrino, Silvia Bua, Fabrizio Carta, Clemente Capasso, Seppo Parkkila & Claudiu T. Supuran
Pages: 1765-1772
Published online: 17 Sep 2020
AbstractforToxicity evaluation of sulfamides and coumarins that efficiently inhibit human carbonic anhydrases | Full Text | References | PDF (2 MB) | EPUB
  • 1301 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
Characterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors
Xia Li, Maowei Ni, Xiaoling Xu & Wei Chen
Pages: 1773-1780
Published online: 20 Sep 2020
AbstractforCharacterisation of naturally occurring isothiocyanates as glutathione reductase inhibitors | Full Text | References | PDF (1.2 MB) | EPUB
  • 1149 Views
  • 7 CrossRef citations
  • 0Altmetric
Open Access
DNA topoisomerases as molecular targets for anticancer drugs
Kamila Buzun, Anna Bielawska, Krzysztof Bielawski & Agnieszka Gornowicz
Pages: 1781-1799
Published online: 25 Sep 2020
AbstractforDNA topoisomerases as molecular targets for anticancer drugs | Full Text | References | PDF (2.8 MB) | EPUB
  • 6199 Views
  • 49 CrossRef citations
  • 0Altmetric
Open Access
Article
The structural basis for the selectivity of sulfonamido dicarbaboranes toward cancer-associated carbonic anhydrase IX
Michael Kugler, Josef Holub, Jiří Brynda, Klára Pospíšilová, Suzan El Anwar, Dmytro Bavol, Miroslav Havránek, Vlastimil Král, Milan Fábry, Bohumír Grüner & Pavlína Řezáčová
Pages: 1800-1810
Published online: 23 Sep 2020
AbstractforThe structural basis for the selectivity of sulfonamido dicarbaboranes toward cancer-associated carbonic anhydrase IX | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1157 Views
  • 8 CrossRef citations
  • 0Altmetric
Open Access
Article
Hydroxypropyl-β-cyclodextrin as an effective carrier of curcumin – piperine nutraceutical system with improved enzyme inhibition properties
Anna Stasiłowicz, Ewa Tykarska, Kornelia Lewandowska, Maciej Kozak, Andrzej Miklaszewski, Joanna Kobus-Cisowska, Daria Szymanowska, Tomasz Plech, Jacek Jenczyk & Judyta Cielecka-Piontek
Pages: 1811-1821
Published online: 23 Sep 2020
AbstractforHydroxypropyl-β-cyclodextrin as an effective carrier of curcumin – piperine nutraceutical system with improved enzyme inhibition properties | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 3316 Views
  • 24 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Structure-activity relationship of 7-aryl-2-anilino-pyrrolopyrimidines as Mer and Axl tyrosine kinase inhibitors
Shin Hyuck Chung, Jiwon Park, Jung Wuk Lee, Jiho Song, Danbee Jung & Kyung Hoon Min
Pages: 1822-1833
Published online: 24 Sep 2020
AbstractforStructure-activity relationship of 7-aryl-2-anilino-pyrrolopyrimidines as Mer and Axl tyrosine kinase inhibitors | Full Text | References | PDF (2.3 MB) | EPUB
  • 1281 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Sulphonamide inhibition profile of Staphylococcus aureus β-carbonic anhydrase
Linda J. Urbanski, Silvia Bua, Andrea Angeli, Marianne Kuuslahti, Vesa. P. Hytönen, Claudiu T. Supuran & Seppo Parkkila
Pages: 1834-1839
Published online: 24 Sep 2020
AbstractforSulphonamide inhibition profile of Staphylococcus aureus β-carbonic anhydrase | Full Text | References | PDF (1.1 MB) | EPUB
  • 1149 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Article
Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation
Jonathan Elie, Omid Feizbakhsh, Nathalie Desban, Béatrice Josselin, Blandine Baratte, Amandine Bescond, Julien Duez, Xavier Fant, Stéphane Bach, Dominique Marie, Matthieu Place, Sami Ben Salah, Agnes Chartier, Sabine Berteina-Raboin, Apirat Chaikuad, Stefan Knapp, Fabrice Carles, Pascal Bonnet, Frédéric Buron, Sylvain Routier & Sandrine Ruchaud
Pages: 1840-1853
Published online: 12 Oct 2020
AbstractforDesign of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 2287 Views
  • 10 CrossRef citations
  • 0Altmetric
Open Access
Article
Design, synthesis, and evaluation of novel N'-substituted-1-(4-chlorobenzyl)-1H-indol-3-carbohydrazides as antitumor agents
Le Cong Huan, Duong Tien Anh, Pham-The Hai, Lai Duc Anh, Eun Jae Park, A Young Ji, Jong Soon Kang, Do Thi Mai Dung, Dao Thi Kim Oanh, Truong Thanh Tung, Dinh Thi Thanh Hai, Sang-Bae Han & Nguyen-Hai Nam
Pages: 1854-1865
Published online: 28 Sep 2020
AbstractforDesign, synthesis, and evaluation of novel N'-substituted-1-(4-chlorobenzyl)-1H-indol-3-carbohydrazides as antitumor agents | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1242 Views
  • 1 CrossRef citations
  • 0Altmetric
Open Access
Article
Inhibition mechanism of naphthylphenylamine derivatives acting on the CDC25B dual phosphatase and analysis of the molecular processes involved in the high cytotoxicity exerted by one selected derivative in melanoma cells
Federica Aliotta, Rosarita Nasso, Rosario Rullo, Alessandro Arcucci, Angelica Avagliano, Martina Simonetti, Gennaro Sanità, Mariorosario Masullo, Antonio Lavecchia, Maria Rosaria Ruocco & Emmanuele De Vendittis
Pages: 1866-1878
Published online: 29 Sep 2020
AbstractforInhibition mechanism of naphthylphenylamine derivatives acting on the CDC25B dual phosphatase and analysis of the molecular processes involved in the high cytotoxicity exerted by one selected derivative in melanoma cells | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 1038 Views
  • 3 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, in vitro inhibitory activity, kinetic study and molecular docking of novel N-alkyl–deoxynojirimycin derivatives as potential α-glucosidase inhibitors
Ping Lin, Jia-Cheng Zeng, Ji-Guang Chen, Xu-Liang Nie, En Yuan, Xiao-Qiang Wang, Da-Yong Peng & Zhong-Ping Yin
Pages: 1879-1890
Published online: 01 Oct 2020
AbstractforSynthesis, in vitro inhibitory activity, kinetic study and molecular docking of novel N-alkyl–deoxynojirimycin derivatives as potential α-glucosidase inhibitors | Full Text | References | PDF (2.2 MB) | EPUB
  • 1415 Views
  • 14 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Novel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation
Paolo Guglielmi, Giulia Rotondi, Daniela Secci, Andrea Angeli, Paola Chimenti, Alessio Nocentini, Alessandro Bonardi, Paola Gratteri, Simone Carradori & Claudiu T. Supuran
Pages: 1891-1905
Published online: 02 Oct 2020
AbstractforNovel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation | Full Text | References | PDF (6.2 MB) | EPUB | Supplemental
  • 1525 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
An overview of carbohydrate-based carbonic anhydrase inhibitors
Doretta Cuffaro, Elisa Nuti & Armando Rossello
Pages: 1906-1922
Published online: 20 Oct 2020
AbstractforAn overview of carbohydrate-based carbonic anhydrase inhibitors | Full Text | References | PDF (4.4 MB)
  • 2709 Views
  • 21 CrossRef citations
  • 0Altmetric
Open Access
Article
Investigation of pesticides on honey bee carbonic anhydrase inhibition
Ercan Soydan, Ahmet Can Olcay, Gürkan Bilir, Ömer Taş, Murat Şentürk, Deniz Ekinci & Claudiu T. Supuran
Pages: 1923-1927
Published online: 20 Oct 2020
AbstractforInvestigation of pesticides on honey bee carbonic anhydrase inhibition | Full Text | References | PDF (727.7 KB)
  • 1310 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Brief Report
Synthesis and biological activity of 2-cyanoacrylamide derivatives tethered to imidazopyridine as TAK1 inhibitors
Seok Jong Kang, Jung Wuk Lee, Jiho Song, Jiwon Park, Jaeyul Choi, Kwee Hyun Suh & Kyung Hoon Min
Pages: 1928-1936
Published online: 22 Oct 2020
AbstractforSynthesis and biological activity of 2-cyanoacrylamide derivatives tethered to imidazopyridine as TAK1 inhibitors | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 1872 Views
  • 2 CrossRef citations
  • 0Altmetric
Open Access
Article
Crystal structure-guided design of berberine-based novel chitinase inhibitors
Lei Chen, Ling Zhu, Jinli Chen, Wei Chen, Xuhong Qian & Qing Yang
Pages: 1937-1943
Published online: 09 Nov 2020
AbstractforCrystal structure-guided design of berberine-based novel chitinase inhibitors | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
  • 1398 Views
  • 12 CrossRef citations
  • 0Altmetric
Open Access
Article
Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer’s disease
Natalia Szałaj, Justyna Godyń, Jakub Jończyk, Anna Pasieka, Dawid Panek, Tomasz Wichur, Krzysztof Więckowski, Paula Zaręba, Marek Bajda, Anja Pislar, Barbara Malawska, Raimon Sabate & Anna Więckowska
Pages: 1944-1952
Published online: 22 Oct 2020
AbstractforMultidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer’s disease | Full Text | References | PDF (3.4 MB) | EPUB
  • 1716 Views
  • 9 CrossRef citations
  • 0Altmetric
Open Access
Article
Scaffold hopping and optimisation of 3’,4’-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H
Graziella Tocco, Francesca Esposito, Pierluigi Caboni, Antonio Laus, John A. Beutler, Jennifer A. Wilson, Angela Corona, Stuart F. J. Le Grice & Enzo Tramontano
Pages: 1953-1963
Published online: 03 Nov 2020
AbstractforScaffold hopping and optimisation of 3’,4’-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 1161 Views
  • 4 CrossRef citations
  • 0Altmetric
Open Access
Article
Synthesis, trehalase hydrolytic resistance and inhibition properties of 4- and 6-substituted trehalose derivatives
Shari Dhaene, Johan Van der Eycken, Koen Beerens, Jorick Franceus, Tom Desmet & Jurgen Caroen
Pages: 1964-1989
Published online: 08 Nov 2020
AbstractforSynthesis, trehalase hydrolytic resistance and inhibition properties of 4- and 6-substituted trehalose derivatives | PDF (4.4 MB) | Supplemental
  • 458 Views
  • 4 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