Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 34, Issue 1 (2019)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 34, Issue 1 (2019)

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Research Paper

Article
Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer
Jonathan Elie, Johnny Vercouillie, Nicolas Arlicot, Lucas Lemaire, Rudy Bidault, Sylvie Bodard, Christel Hosselet, Jean-Bernard Deloye, Sylvie Chalon, Patrick Emond, Denis Guilloteau, Frédéric Buron & Sylvain Routier
Pages: 1-7
Published online: 26 Oct 2018
AbstractforDesign of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2373 Views
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Open Access
Article
Phosphonate inhibitors of West Nile virus NS2B/NS3 protease
Marcin Skoreński, Aleksandra Milewska, Krzysztof Pyrć, Marcin Sieńczyk & Józef Oleksyszyn
Pages: 8-14
Published online: 26 Oct 2018
AbstractforPhosphonate inhibitors of West Nile virus NS2B/NS3 protease | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 3028 Views
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Open Access
Article
Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents
Yuheng Hu, Bing Wang, Jie Yang, Teng Liu, Jie Sun & Xiaojing Wang
Pages: 15-30
Published online: 26 Oct 2018
AbstractforSynthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 3296 Views
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Open Access
Article
Refining the structure−activity relationships of 2-phenylcyclopropane carboxylic acids as inhibitors of O-acetylserine sulfhydrylase isoforms
Joana Magalhães, Nina Franko, Giannamaria Annunziato, Marco Pieroni, Roberto Benoni, Anna Nikitjuka, Andrea Mozzarelli, Stefano Bettati, Anna Karawajczyk, Aigars Jirgensons, Barbara Campanini & Gabriele Costantino
Pages: 31-43
Published online: 26 Oct 2018
AbstractforRefining the structure−activity relationships of 2-phenylcyclopropane carboxylic acids as inhibitors of O-acetylserine sulfhydrylase isoforms | Full Text | References | PDF (1.3 MB) | EPUB
  • 1904 Views
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Open Access

Short Communication

Rapid Communication
iVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancer
Agostino Cilibrizzi, Giuseppe Floresta, Vincenzo Abbate & Maria Paola Giovannoni
Pages: 44-50
Published online: 26 Oct 2018
AbstractforiVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancer | Full Text | References | PDF (945.4 KB) | EPUB | Supplemental
  • 1265 Views
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Open Access

Research Paper

Article
Determination of the inhibitory effects of N-methylpyrrole derivatives on glutathione reductase enzyme
Esma Kocaoğlu, Oktay Talaz, Hüseyin Çavdar, Murat Şentürk, Claudiu T. Supuran & Deniz Ekinci
Pages: 51-54
Published online: 26 Oct 2018
AbstractforDetermination of the inhibitory effects of N-methylpyrrole derivatives on glutathione reductase enzyme | Full Text | References | PDF (722.5 KB) | EPUB
  • 1872 Views
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Open Access
Article
From cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitors
Serena Massari, Angela Corona, Simona Distinto, Jenny Desantis, Alessia Caredda, Stefano Sabatini, Giuseppe Manfroni, Tommaso Felicetti, Violetta Cecchetti, Christophe Pannecouque, Elias Maccioni, Enzo Tramontano & Oriana Tabarrini
Pages: 55-74
Published online: 26 Oct 2018
AbstractforFrom cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitors | Full Text | References | PDF (3 MB) | EPUB
  • 1981 Views
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Open Access
Article
Assessment of the antiproliferative and apoptotic roles of sulfonamide carbonic anhydrase IX inhibitors in HeLa cancer cell line
Ismail Koyuncu, Ataman Gonel, Mustafa Durgun, Abdurrahim Kocyigit, Ozgur Yuksekdag & Claudiu T. Supuran
Pages: 75-86
Published online: 26 Oct 2018
AbstractforAssessment of the antiproliferative and apoptotic roles of sulfonamide carbonic anhydrase IX inhibitors in HeLa cancer cell line | Full Text | References | PDF (2.3 MB)
  • 2556 Views
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Open Access
Article
Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3
M. Lourdes Sciú, Victor Sebastián-Pérez, Loreto Martinez-Gonzalez, Rocio Benitez, Daniel I. Perez, Concepción Pérez, Nuria E. Campillo, Ana Martinez & E. Laura Moyano
Pages: 87-96
Published online: 26 Oct 2018
AbstractforComputer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3 | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 2164 Views
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Open Access
Article
Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety
Mohammed S. Abdel-Maksoud, Mohammed I. El-Gamal, Mahmoud M. Gamal El-Din & Chang Hyun Oh
Pages: 97-109
Published online: 26 Oct 2018
AbstractforDesign, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2064 Views
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Open Access
Article
Synthesis and cytotoxic activities of novel copper and silver complexes of 1,3-diaryltriazene-substituted sulfonamides
Dilek Canakci, Ismail Koyuncu, Nabih Lolak, Mustafa Durgun, Suleyman Akocak & Claudiu T. Supuran
Pages: 110-116
Published online: 26 Oct 2018
AbstractforSynthesis and cytotoxic activities of novel copper and silver complexes of 1,3-diaryltriazene-substituted sulfonamides | Full Text | References | PDF (1.1 MB) | EPUB
  • 2844 Views
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Open Access
Article
The carbonic anhydrase IX inhibitor SLC-0111 sensitises cancer cells to conventional chemotherapy
Elena Andreucci, Jessica Ruzzolini, Silvia Peppicelli, Francesca Bianchini, Anna Laurenzana, Fabrizio Carta, Claudiu T. Supuran & Lido Calorini
Pages: 117-123
Published online: 26 Oct 2018
AbstractforThe carbonic anhydrase IX inhibitor SLC-0111 sensitises cancer cells to conventional chemotherapy | Full Text | References | PDF (1 MB) | EPUB
  • 4209 Views
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Open Access

Short Communication

Rapid Communication
Synthesis of novel 6,7-dimethoxy-4-anilinoquinolines as potent c-Met inhibitors
Qing-Wen Zhang, Zi-Dan Ye, Chang Shen, Hong-Xia Tie, Lei Wang & Lei Shi
Pages: 124-133
Published online: 13 Nov 2018
AbstractforSynthesis of novel 6,7-dimethoxy-4-anilinoquinolines as potent c-Met inhibitors | Full Text | References | PDF (1.4 MB) | EPUB
  • 1983 Views
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Research Paper

Article
Computational screening of chalcones acting against topoisomerase IIα and their cytotoxicity towards cancer cell lines
Kanyani Sangpheak, Monika Mueller, Nitchakan Darai, Peter Wolschann, Chonticha Suwattanasophon, Ritbey Ruga, Warinthon Chavasiri, Supaporn Seetaha, Kiattawee Choowongkomon, Nawee Kungwan, Chompoonut Rungnim & Thanyada Rungrotmongkol
Pages: 134-143
Published online: 04 Nov 2018
AbstractforComputational screening of chalcones acting against topoisomerase IIα and their cytotoxicity towards cancer cell lines | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 2883 Views
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Short Communication

Rapid Communication
HPLC–UV assay for the evaluation of inhibitors of plasma amine oxidase using crude bovine plasma
Kira Mergemeier, Florian Galster & Matthias Lehr
Pages: 144-149
Published online: 14 Nov 2018
AbstractforHPLC–UV assay for the evaluation of inhibitors of plasma amine oxidase using crude bovine plasma | Full Text | References | PDF (681.5 KB) | EPUB
  • 1482 Views
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Research Paper

Article
Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors
Cheng-Zhi Gao, Wei Dong, Zhi-Wen Cui, Qiong Yuan, Xia-Min Hu, Qing-Ming Wu, Xianlin Han, Yao Xu & Zhen-Li Min
Pages: 150-162
Published online: 14 Nov 2018
AbstractforSynthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 4253 Views
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Short Communication

Rapid Communication
Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer’s disease therapy
Youssef Dgachi, Hélène Martin, Rim Malek, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Isabel Iriepa, Ignacio Moraleda, Emna Maalej, M. Carmo Carreiras, Bernard Refouvelet, Fakher Chabchoub, José Marco-Contelles & Lhassane Ismaili
Pages: 163-170
Published online: 27 Nov 2018
AbstractforSynthesis and biological assessment of KojoTacrines as new agents for Alzheimer’s disease therapy | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
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Open Access

Research Paper

Article
Repurposing existing drugs: identification of irreversible IMPDH inhibitors by high-throughput screening
Albertus Eka Yudistira Sarwono, Shinya Mitsuhashi, Mohammad Hazzaz Bin Kabir, Kengo Shigetomi, Tadashi Okada, Fumina Ohsaka, Satoko Otsuguro, Katsumi Maenaka, Makoto Igarashi, Kentaro Kato & Makoto Ubukata
Pages: 171-178
Published online: 19 Nov 2018
AbstractforRepurposing existing drugs: identification of irreversible IMPDH inhibitors by high-throughput screening | Full Text | References | PDF (1,005.1 KB) | EPUB | Supplemental
  • 2988 Views
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Open Access
Article
Carbonic anhydrase 12 mutation modulates membrane stability and volume regulation of aquaporin 5
Soyoung Hwang, Jung Yun Kang, Min Jae Kim, Dong Min Shin & Jeong Hee Hong
Pages: 179-188
Published online: 19 Nov 2018
AbstractforCarbonic anhydrase 12 mutation modulates membrane stability and volume regulation of aquaporin 5 | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1794 Views
  • 10 CrossRef citations
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Open Access
Article
Identification and characterization of the α-CA in the outer membrane vesicles produced by Helicobacter pylori
Maurizio Ronci, Sonia Del Prete, Valentina Puca, Simone Carradori, Vincenzo Carginale, Raffaella Muraro, Gabriella Mincione, Antonio Aceto, Francesca Sisto, Claudiu T. Supuran, Rossella Grande & Clemente Capasso
Pages: 189-195
Published online: 07 Jan 2019
AbstractforIdentification and characterization of the α-CA in the outer membrane vesicles produced by Helicobacter pylori | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1769 Views
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Short Communication

Rapid Communication
Synthesis and biological evaluation of benzothiazin-4-ones: a possible new class of acetylcholinesterase inhibitors
Gabriele A. Berwaldt, Daniela P. Gouvêa, Daniel S. da Silva, Adriana M. das Neves, Mayara S. P. Soares, Juliana H. Azambuja, Geonir M. Siqueira, Roselia M. Spanevello & Wilson Cunico
Pages: 196-202
Published online: 27 Nov 2018
AbstractforSynthesis and biological evaluation of benzothiazin-4-ones: a possible new class of acetylcholinesterase inhibitors | Full Text | References | PDF (999.9 KB) | EPUB
  • 1599 Views
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Open Access

Original Article

Article
Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers
Caolin Wang, Shan Xu, Liang Peng, Bingliang Zhang, Hong Zhang, Yingying Hu, Pengwu Zheng & Wufu Zhu
Pages: 203-217
Published online: 04 Dec 2018
AbstractforDesign, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 2254 Views
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Open Access

Short Communication

Rapid Communication
Comparison of blood carbonic anhydrase activity of athletes performing interval and continuous running exercise at high altitude
Murat Tas, Esra Senturk, Deniz Ekinci, Ramazan Demirdag, Veysal Comakli, Metin Bayram, Murat Akyuz, Murat Senturk & Claudiu T. Supuran
Pages: 218-223
Published online: 06 Dec 2018
AbstractforComparison of blood carbonic anhydrase activity of athletes performing interval and continuous running exercise at high altitude | Full Text | References | PDF (843.5 KB) | EPUB
  • 2676 Views
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Open Access

Research Paper

Article
(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
Marouan Rami, Jean-Yves Winum, Claudiu T. Supuran, Patricia Melnyk & Saïd Yous
Pages: 224-229
Published online: 03 Jan 2019
Abstractfor(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators | Full Text | References | PDF (870.7 KB) | EPUB
  • 1200 Views
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Open Access
Article
Synthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivatives
Lacramioara Popovici, Roxana-Maria Amarandi, Ionel I. Mangalagiu, Violeta Mangalagiu & Ramona Danac
Pages: 230-243
Published online: 03 Jan 2019
AbstractforSynthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivatives | Full Text | References | PDF (1.8 MB) | EPUB
  • 1908 Views
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Short Communication

Rapid Communication
Inhibition of bacterial α-, β- and γ-class carbonic anhydrases with selenazoles incorporating benzenesulfonamide moieties
Andrea Angeli, Mariana Pinteala, Stelian S. Maier, Sonia Del Prete, Clemente Capasso, Bogdan C. Simionescu & Claudiu T. Supuran
Pages: 244-249
Published online: 27 Dec 2018
AbstractforInhibition of bacterial α-, β- and γ-class carbonic anhydrases with selenazoles incorporating benzenesulfonamide moieties | Full Text | References | PDF (1.1 MB) | EPUB
  • 1367 Views
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Research Paper

Article
Discovery of cyanopyridine scaffold as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors through virtual screening and preliminary hit optimisation
Xi Xu, Jie Ren, Yinghe Ma, Hongting Liu, Quanjin Rong, Yifan Feng, Yameng Wang, Yu Cheng, Ruijia Ge, Zhiyu Li & Jinlei Bian
Pages: 250-263
Published online: 02 Jan 2019
AbstractforDiscovery of cyanopyridine scaffold as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors through virtual screening and preliminary hit optimisation | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 2817 Views
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Open Access
Article
Hydroxyl-substituted double Schiff-base condensed 4-piperidone/cyclohexanones as potential anticancer agents with biological evaluation
Lianshuang Zhang, Qin Chen, Guige Hou, Wei Zhao & Yun Hou
Pages: 264-271
Published online: 02 Jan 2019
AbstractforHydroxyl-substituted double Schiff-base condensed 4-piperidone/cyclohexanones as potential anticancer agents with biological evaluation | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
  • 1755 Views
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Open Access
Article
Prostate cancer cells and exosomes in acidic condition show increased carbonic anhydrase IX expression and activity
Mariantonia Logozzi, Clemente Capasso, Rossella Di Raimo, Sonia Del Prete, Davide Mizzoni, Mario Falchi, Claudiu T. Supuran & Stefano Fais
Pages: 272-278
Published online: 02 Jan 2019
AbstractforProstate cancer cells and exosomes in acidic condition show increased carbonic anhydrase IX expression and activity | Full Text | References | PDF (1 MB) | Supplemental
  • 2420 Views
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Open Access

Review Article

Review
A comprehensive review on tyrosinase inhibitors
Samaneh Zolghadri, Asieh Bahrami, Mahmud Tareq Hassan Khan, J. Munoz-Munoz, F. Garcia-Molina, F. Garcia-Canovas & Ali Akbar Saboury
Pages: 279-309
Published online: 03 Jan 2019
AbstractforA comprehensive review on tyrosinase inhibitors | Full Text | References | PDF (3.4 MB) | EPUB
  • 45089 Views
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Research Paper

Article
Targeting Loxosceles spider Sphingomyelinase D with small-molecule inhibitors as a potential therapeutic approach for loxoscelism
Priscila Hess Lopes, Mário T. Murakami, Fernanda C. V. Portaro, Kerly Fernanda Mesquita Pasqualoto, Carmen van den Berg & Denise V. Tambourgi
Pages: 310-321
Published online: 07 Jan 2019
AbstractforTargeting Loxosceles spider Sphingomyelinase D with small-molecule inhibitors as a potential therapeutic approach for loxoscelism | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 2081 Views
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Open Access
Article
Synthesis and in vitro anticancer activity of certain novel 1-(2-methyl-6-arylpyridin-3-yl)-3-phenylureas as apoptosis-inducing agents
Wagdy M. Eldehna, Ghada S. Hassan, Sara T. Al-Rashood, Tarfah Al-Warhi, Ahmed E. Altyar, Hamad M. Alkahtani, Abdulrahman A. Almehizia & Hatem A. Abdel-Aziz
Pages: 322-332
Published online: 05 Feb 2019
AbstractforSynthesis and in vitro anticancer activity of certain novel 1-(2-methyl-6-arylpyridin-3-yl)-3-phenylureas as apoptosis-inducing agents | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2566 Views
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Open Access
Article
Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors
Camila C. Bitencourt Brito, Hélder Vinicius Carneiro da Silva, Daci José Brondani, Antonio Rodolfo de Faria, Rafael Matos Ximenes, Ivanildo Mangueira da Silva, Julianna F. C. de Albuquerque & Marcelo Santos Castilho
Pages: 333-342
Published online: 27 Dec 2018
AbstractforSynthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors | Full Text | References | PDF (1.1 MB) | EPUB
  • 2149 Views
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Open Access
Article
Synthesis carbonic anhydrase enzyme inhibition and antioxidant activity of novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine moieties
Deniz Üzeroğlu Payaz, F. Zehra Küçükbay, Hasan Küçükbay, Andrea Angeli & Claudiu T. Supuran
Pages: 343-349
Published online: 27 Dec 2018
AbstractforSynthesis carbonic anhydrase enzyme inhibition and antioxidant activity of novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine moieties | Full Text | References | PDF (1.4 MB) | EPUB
  • 1615 Views
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Open Access
Article
Soyasaponins from Zolfino bean as aldose reductase differential inhibitors
Francesco Balestri, Marinella De Leo, Carlo Sorce, Mario Cappiello, Luca Quattrini, Roberta Moschini, Carlotta Pineschi, Alessandra Braca, Concettina La Motta, Federico Da Settimo, Antonella Del-Corso & Umberto Mura
Pages: 350-360
Published online: 27 Dec 2018
AbstractforSoyasaponins from Zolfino bean as aldose reductase differential inhibitors | Full Text | References | PDF (1.4 MB) | EPUB
  • 1427 Views
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Review Article

Review
The chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1
Xinyuan Xu, Yingyi Chen, Qiang Fu, Duan Ni, Jian Zhang, Xiaolong Li & Shaoyong Lu
Pages: 361-374
Published online: 03 Jan 2019
AbstractforThe chemical diversity and structure-based discovery of allosteric modulators for the PIF-pocket of protein kinase PDK1 | Full Text | References | PDF (2.4 MB) | EPUB
  • 2948 Views
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Research Paper

Article
Synthesis and biological evaluation of novel N9-heterobivalent β-carbolines as angiogenesis inhibitors
Liang Guo, Qin Ma, Wei Chen, Wenxi Fan, Jie Zhang & Bin Dai
Pages: 375-387
Published online: 02 Jan 2019
AbstractforSynthesis and biological evaluation of novel N9-heterobivalent β-carbolines as angiogenesis inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1662 Views
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Short Communication

Rapid Communication
Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII
Sara Seršen, Katja Traven, Jakob Kljun, Iztok Turel & Claudiu T. Supuran
Pages: 388-393
Published online: 03 Jan 2019
AbstractforOrganoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII | Full Text | References | PDF (786.9 KB) | EPUB
  • 1662 Views
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Research Paper

Article
A mitochondrial-targeted peptide ameliorated podocyte apoptosis through a HOCl-alb-enhanced and mitochondria-dependent signalling pathway in diabetic rats and in vitro
Xiaoqiao Wang, Dongdong Tang, Yaowei Zou, Xiaoyu Wu, Yihua Chen, Hongying Li, Siqi Chen, Yue Shi & Hongxin Niu
Pages: 394-404
Published online: 07 Jan 2019
AbstractforA mitochondrial-targeted peptide ameliorated podocyte apoptosis through a HOCl-alb-enhanced and mitochondria-dependent signalling pathway in diabetic rats and in vitro | Full Text | References | PDF (1.5 MB) | EPUB
  • 2104 Views
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Review Article

Review
Trypsin inhibitors: promising candidate satietogenic proteins as complementary treatment for obesity and metabolic disorders?
Vanessa Cristina Oliveira de Lima, Grasiela Piuvezam, Bruna Leal Lima Maciel & Ana Heloneida de Araújo Morais
Pages: 405-419
Published online: 07 Jan 2019
AbstractforTrypsin inhibitors: promising candidate satietogenic proteins as complementary treatment for obesity and metabolic disorders? | Full Text | References | PDF (1.2 MB) | EPUB
  • 4386 Views
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Research Paper

Article
A feature-based analysis identifies COL1A2 as a regulator in pancreatic cancer
Jie Wu, Jing Liu, XiaoQing Wei, Qi Yu, XiangHuan Niu, ShuHong Tang & Lei Song
Pages: 420-428
Published online: 07 Jan 2019
AbstractforA feature-based analysis identifies COL1A2 as a regulator in pancreatic cancer | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 2001 Views
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Open Access
Article
Inhibition of acetylcholinesterase and butyrylcholinesterase with uracil derivatives: kinetic and computational studies
Huseyin Cavdar, Murat Senturk, Murat Guney, Serdar Durdagi, Gulru Kayik, Claudiu T. Supuran & Deniz Ekinci
Pages: 429-437
Published online: 07 Jan 2019
AbstractforInhibition of acetylcholinesterase and butyrylcholinesterase with uracil derivatives: kinetic and computational studies | Full Text | References | PDF (1.4 MB) | EPUB
  • 4669 Views
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Open Access
Article
Structure-guided design of anti-cancer ribonucleotide reductase inhibitors
Tessianna A. Misko, Yi-Ting Liu, Michael E. Harris, Nancy L. Oleinick, John Pink, Hsueh-Yun Lee & Chris G. Dealwis
Pages: 438-450
Published online: 07 Jan 2019
AbstractforStructure-guided design of anti-cancer ribonucleotide reductase inhibitors | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 2681 Views
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Open Access
Article
New sulfonamides containing organometallic-acylhydrazones: synthesis, characterisation and biological evaluation as inhibitors of human carbonic anhydrases
Yosselin Huentupil, Luis Peña, Néstor Novoa, Emanuela Berrino, Rodrigo Arancibia & Claudiu T. Supuran
Pages: 451-458
Published online: 07 Jan 2019
AbstractforNew sulfonamides containing organometallic-acylhydrazones: synthesis, characterisation and biological evaluation as inhibitors of human carbonic anhydrases | Full Text | References | PDF (1 MB)
  • 1539 Views
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Article
Do CO2 and oxidative stress induce cancer?: a brief study about the evaluation of PON 1, CAT, CA and XO enzyme levels on head and neck cancer patients
Murad Mutlu, M. Hakan Korkmaz, Ender Simsek, Emine Terzi, Beyza Ecem Oz Bedir, Tugba Kevser Uysal, Omer Bayir, Guleser Saylam & Ozen Ozensoy Guler
Pages: 459-464
Published online: 03 Jan 2019
AbstractforDo CO2 and oxidative stress induce cancer?: a brief study about the evaluation of PON 1, CAT, CA and XO enzyme levels on head and neck cancer patients | Full Text | References | PDF (634.7 KB) | EPUB
  • 1888 Views
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Article
(E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activity
Le Cong Huan, Cao Viet Phuong, Le Cong Truc, Vo Nguyen Thanh, Hai Pham-The, Le-Thi-Thu Huong, Nguyen Thi Thuan, Eun Jae Park, A Young Ji, Jong Soon Kang, Sang-Bae Han, Phuong-Thao Tran & Nguyen-Hai Nam
Pages: 465-478
Published online: 17 Jan 2019
Abstractfor(E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activity | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1887 Views
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Short Communication

Rapid Communication
Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer’s disease therapy
Irene Pachón-Angona, Bernard Refouvelet, Rudolf Andrýs, Helène Martin, Vincent Luzet, Isabel Iriepa, Ignacio Moraleda, Daniel Diez-Iriepa, María-Jesús Oset-Gasque, José Marco-Contelles, Kamil Musilek & Lhassane Ismaili
Pages: 479-489
Published online: 04 Feb 2019
AbstractforDonepezil + chromone + melatonin hybrids as promising agents for Alzheimer’s disease therapy | Full Text | References | PDF (2 MB) | EPUB | Supplemental
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Article
An AGT-based protein-tag system for the labelling and surface immobilization of enzymes on E. coli outer membrane
Rosa Merlo, Sonia Del Prete, Anna Valenti, Rosanna Mattossovich, Vincenzo Carginale, Claudiu T. Supuran, Clemente Capasso & Giuseppe Perugino
Pages: 490-499
Published online: 06 Feb 2019
AbstractforAn AGT-based protein-tag system for the labelling and surface immobilization of enzymes on E. coli outer membrane | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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Article
Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems
Zoltán Kónya, Bálint Bécsi, Andrea Kiss, Dániel Horváth, Mária Raics, Katalin E. Kövér, Beáta Lontay & Ferenc Erdődi
Pages: 500-509
Published online: 30 Jan 2019
AbstractforInhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems | Full Text | References | PDF (1.2 MB) | EPUB
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Article
Phaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors
Alessandra Rogato, Sonia Del Prete, Alessio Nocentini, Vincenzo Carginale, Claudiu T. Supuran & Clemente Capasso
Pages: 510-518
Published online: 27 Jan 2019
AbstractforPhaeodactylum tricornutum as a model organism for testing the membrane penetrability of sulphonamide carbonic anhydrase inhibitors | Full Text | References | PDF (1.3 MB) | EPUB
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Article
Chemical composition and enzyme inhibition of Phytolacca dioica L. seeds extracts
Amalia Di Petrillo, Ana María González-Paramás, Antonella Rosa, Valeria Ruggiero, Fabio Boylan, Amit Kumar, Francesca Pintus, Celestino Santos-Buelga, Antonella Fais & Benedetta Era
Pages: 519-527
Published online: 27 Jan 2019
AbstractforChemical composition and enzyme inhibition of Phytolacca dioica L. seeds extracts | Full Text | References | PDF (896.5 KB) | EPUB
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Article
Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme
Atilla Akdemir, Andrea Angeli, Füsun Göktaş, Pınar Eraslan Elma, Nilgün Karalı & Claudiu T. Supuran
Pages: 528-531
Published online: 06 Feb 2019
AbstractforNovel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme | Full Text | References | PDF (877 KB) | EPUB
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Novel pyrazolo[3,4-d]pyrimidines: design, synthesis, anticancer activity, dual EGFR/ErbB2 receptor tyrosine kinases inhibitory activity, effects on cell cycle profile and caspase-3-mediated apoptosis
Mai Maher, Asmaa E. Kassab, Ashraf F. Zaher & Zeinab Mahmoud
Pages: 532-546
Published online: 27 Jan 2019
AbstractforNovel pyrazolo[3,4-d]pyrimidines: design, synthesis, anticancer activity, dual EGFR/ErbB2 receptor tyrosine kinases inhibitory activity, effects on cell cycle profile and caspase-3-mediated apoptosis | Full Text | References | PDF (1.9 MB) | EPUB
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Article
Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone–chalcone and isatin–chalcone inhibitors probing the S2 active site pocket
Koffi N’Guessan Placide Gabin Allangba, Mélalie Keita, Raymond Kre N’Guessan, Eugene Megnassan, Vladimir Frecer & Stanislav Miertus
Pages: 547-561
Published online: 30 Jan 2019
AbstractforVirtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone–chalcone and isatin–chalcone inhibitors probing the S2 active site pocket | Full Text | References | PDF (1.9 MB) | EPUB
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Article
Benzylamides and piperazinoarylamides of ibuprofen as fatty acid amide hydrolase inhibitors
Alessandro Deplano, Mariateresa Cipriano, Federica Moraca, Ettore Novellino, Bruno Catalanotti, Christopher J. Fowler & Valentina Onnis
Pages: 562-576
Published online: 27 Jan 2019
AbstractforBenzylamides and piperazinoarylamides of ibuprofen as fatty acid amide hydrolase inhibitors | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
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Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
Carina Proença, Marisa Freitas, Daniela Ribeiro, Sara M. Tomé, Eduardo F. T. Oliveira, Matilde F. Viegas, Alberto N. Araújo, Maria J. Ramos, Artur M. S. Silva, Pedro A. Fernandes & Eduarda Fernandes
Pages: 577-588
Published online: 06 Feb 2019
AbstractforEvaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
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Rapid Communication
Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors
Giulio Poli, Margherita Lapillo, Vibhu Jha, Nayla Mouawad, Isabella Caligiuri, Marco Macchia, Filippo Minutolo, Flavio Rizzolio, Tiziano Tuccinardi & Carlotta Granchi
Pages: 589-596
Published online: 30 Jan 2019
AbstractforComputationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
Daniela Secci, Simone Carradori, Anél Petzer, Paolo Guglielmi, Melissa D’Ascenzio, Paola Chimenti, Donatella Bagetta, Stefano Alcaro, Gokhan Zengin, Jacobus P. Petzer & Francesco Ortuso
Pages: 597-612
Published online: 06 Feb 2019
Abstractfor4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis | Full Text | References | PDF (2.3 MB) | EPUB
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Article
Effect of cinnamamides on atopic dermatitis through regulation of IL-4 in CD4+ cells
Eun-Ju Choi, Young Bae Ryu, Yujiao Tang, Bo Ram Kim, Woo Song Lee, Trishna Debnath, Meiqi Fan, Hyun-Su Lee & Eun-Kyung Kim
Pages: 613-619
Published online: 06 Feb 2019
AbstractforEffect of cinnamamides on atopic dermatitis through regulation of IL-4 in CD4+ cells | Full Text | References | PDF (909.3 KB) | EPUB
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Article
Design and synthesis of 4-piperazinyl quinoline derived urea/thioureas for anti-breast cancer activity by a hybrid pharmacophore approach
Raja Solomon Viswas, Sheetal Pundir & Hoyun Lee
Pages: 620-630
Published online: 06 Feb 2019
AbstractforDesign and synthesis of 4-piperazinyl quinoline derived urea/thioureas for anti-breast cancer activity by a hybrid pharmacophore approach | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
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Rapid Communication
Discovery of novel dual-active 3-(4-(dimethylamino)phenyl)-7-aminoalcoxy-coumarin as potent and selective acetylcholinesterase inhibitor and antioxidant
Gabriela Alves de Souza, Soraia John da Silva, Catarina de Nigris Del Cistia, Paulo Pitasse-Santos, Lucas de Oliveira Pires, Yulli Moraes Passos, Yraima Cordeiro, Cristiane Martins Cardoso, Rosane Nora Castro, Carlos Mauricio R. Sant’Anna & Arthur Eugen Kümmerle
Pages: 631-637
Published online: 06 Feb 2019
AbstractforDiscovery of novel dual-active 3-(4-(dimethylamino)phenyl)-7-aminoalcoxy-coumarin as potent and selective acetylcholinesterase inhibitor and antioxidant | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Rapid Communication
Development of a novel, high-affinity ssDNA trypsin inhibitor
Stanislaw Malicki, Miroslaw Ksiazek, Pawel Majewski, Aleksandra Pecak, Piotr Mydel, Przemyslaw Grudnik & Grzegorz Dubin
Pages: 638-643
Published online: 06 Feb 2019
AbstractforDevelopment of a novel, high-affinity ssDNA trypsin inhibitor | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
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Inhibition of α-, β-, γ-, δ-, ζ- and η-class carbonic anhydrases from bacteria, fungi, algae, diatoms and protozoans with famotidine
Andrea Angeli, Mariana Pinteala, Stelian S. Maier, Sonia Del Prete, Clemente Capasso, Bogdan C. Simionescu & Claudiu T. Supuran
Pages: 644-650
Published online: 07 Feb 2019
AbstractforInhibition of α-, β-, γ-, δ-, ζ- and η-class carbonic anhydrases from bacteria, fungi, algae, diatoms and protozoans with famotidine | Full Text | References | PDF (1.2 MB) | EPUB
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Article
Synthesis and biological evaluation of 3-arylcoumarins as potential anti-Alzheimer's disease agents
Jie Yang, Pingping Zhang, Yuheng Hu, Teng Liu, Jie Sun & Xiaojing Wang
Pages: 651-656
Published online: 12 Feb 2019
AbstractforSynthesis and biological evaluation of 3-arylcoumarins as potential anti-Alzheimer's disease agents | Full Text | References | PDF (1 MB) | EPUB
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Article
Chemically stable inhibitors of 14-3-3 protein–protein interactions derived from BV02
Leire Iralde-Lorente, Ylenia Cau, Letizia Clementi, Lorenzo Franci, Giusy Tassone, Daniela Valensin, Mattia Mori, Adriano Angelucci, Mario Chiariello & Maurizio Botta
Pages: 657-664
Published online: 07 Feb 2019
AbstractforChemically stable inhibitors of 14-3-3 protein–protein interactions derived from BV02 | Full Text | References | PDF (1.1 MB) | EPUB
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Design, synthesis, and biological evaluation of novel derivatives of dithiodiglycolic acid prepared via oxidative coupling of thiols
Olga Bakulina, Anton Bannykh, Mirna Jovanović, Ilona Domračeva, Ana Podolski-Renić, Raivis Žalubovskis, Milica Pešić, Dmitry Dar’in & Mikhail Krasavin
Pages: 665-671
Published online: 12 Feb 2019
AbstractforDesign, synthesis, and biological evaluation of novel derivatives of dithiodiglycolic acid prepared via oxidative coupling of thiols | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Article
Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
Nahed N. E. El-Sayed, Norah M. Almaneai, Abir Ben Bacha, Omar Al-Obeed, Rehan Ahmad, Maha Abdulla & Ahmed M. Alafeefy
Pages: 672-683
Published online: 01 Mar 2019
AbstractforSynthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
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Article
In vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts
Ghina Alameh, Agnès Emptoz-Bonneton, Marc Rolland de Ravel, Eva L. Matera, Elisabeth Mappus, Patrick Balaguer, Luc Rocheblave, Thierry Lomberget, Charles Dumontet, Marc Le Borgne, Michel Pugeat, Catherine Grenot & Claude Y. Cuilleron
Pages: 684-691
Published online: 19 Feb 2019
AbstractforIn vitro modulation of multidrug resistance by pregnane steroids and in vivo inhibition of tumour development by 7α-OBz-11α(R)-OTHP-5β-pregnanedione in K562/R7 and H295R cell xenografts | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Article
Aberrant regulation favours matriptase proteolysis in neoplastic B-cells that co-express HAI-2
Yi-Lin Chiu, Yi-Ying Wu, Robert B. Barndt, Yee Hui Yeo, Yu-Wen Lin, Hou-Ping Sytwo, Huan-Cheng Liu, Yuan Xu, Bailing Jia, Jehng-Kang Wang, Michael D. Johnson & Chen-Yong Lin
Pages: 692-702
Published online: 19 Feb 2019
AbstractforAberrant regulation favours matriptase proteolysis in neoplastic B-cells that co-express HAI-2 | Full Text | References | PDF (1.4 MB) | EPUB
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Article
Evaluation of the anticancer potential of a sulphonamide carbonic anhydrase IX inhibitor on cervical cancer cells
Ismail Koyuncu, Yasin Tülüce, Hewa Slahaddin Qadir, Mustafa Durgun & Claudiu T. Supuran
Pages: 703-711
Published online: 27 Feb 2019
AbstractforEvaluation of the anticancer potential of a sulphonamide carbonic anhydrase IX inhibitor on cervical cancer cells | Full Text | References | PDF (1.4 MB)
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Article
New flavonoid – N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic properties
Martín Estrada-Valencia, Clara Herrera-Arozamena, Concepción Pérez, Dolores Viña, José A. Morales-García, Ana Pérez-Castillo, Eva Ramos, Alejandro Romero, Erik Laurini, Sabrina Pricl & María Isabel Rodríguez-Franco
Pages: 712-727
Published online: 07 Mar 2019
AbstractforNew flavonoid – N,N-dibenzyl(N-methyl)amine hybrids: Multi-target-directed agents for Alzheimer´s disease endowed with neurogenic properties | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Delivering bioactive cyclic peptides that target Hsp90 as prodrugs
Yuantao Huo, Laura K. Buckton, Jack L. Bennett, Eloise C. Smith, Frances L. Byrne, Kyle L. Hoehn, Marwa N. Rahimi & Shelli R. McAlpine
Pages: 728-739
Published online: 01 Mar 2019
AbstractforDelivering bioactive cyclic peptides that target Hsp90 as prodrugs | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Article
Exploring the activity of polyamine analogues on polyamine and spermine oxidase: methoctramine, a potent and selective inhibitor of polyamine oxidase
Maria Luisa Di Paolo, Manuela Cervelli, Paolo Mariottini, Alessia Leonetti, Fabio Polticelli, Michela Rosini, Andrea Milelli, Filippo Basagni, Rina Venerando, Enzo Agostinelli & Anna Minarini
Pages: 740-752
Published online: 04 Mar 2019
AbstractforExploring the activity of polyamine analogues on polyamine and spermine oxidase: methoctramine, a potent and selective inhibitor of polyamine oxidase | Full Text | References | PDF (3.3 MB) | EPUB
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Article
Inhibition potential of phenolic constituents from the aerial parts of Tetrastigma hemsleyanum against soluble epoxide hydrolase and nitric oxide synthase
Cai Yi Wang, Sunggun Lee, Hyun-Jae Jang, Xiang Dong Su, Heng-Shan Wang, Young Ho Kim & Seo Young Yang
Pages: 753-760
Published online: 04 Mar 2019
AbstractforInhibition potential of phenolic constituents from the aerial parts of Tetrastigma hemsleyanum against soluble epoxide hydrolase and nitric oxide synthase | Full Text | References | PDF (1 MB) | EPUB | Supplemental
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Article
Synthesis and biological evaluation of ursolic acid derivatives bearing triazole moieties as potential anti-Toxoplasma gondii agents
Tian Luan, Chunmei Jin, Chun-Mei Jin, Guo-Hua Gong & Zhe-Shan Quan
Pages: 761-772
Published online: 05 Mar 2019
AbstractforSynthesis and biological evaluation of ursolic acid derivatives bearing triazole moieties as potential anti-Toxoplasma gondii agents | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
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Novel Re(I) tricarbonyl coordination compounds based on 2-pyridyl-1,2,3-triazole derivatives bearing a 4-amino-substituted benzenesulfonamide arm: synthesis, crystal structure, computational studies and inhibitory activity against carbonic anhydrase I, II, and IX isoforms†
Yassine Aimene, Romain Eychenne, Sonia Mallet-Ladeira, Nathalie Saffon, Jean-Yves Winum, Alessio Nocentini, Claudiu T. Supuran, Eric Benoist & Achour Seridi
Pages: 773-782
Published online: 07 Mar 2019
AbstractforNovel Re(I) tricarbonyl coordination compounds based on 2-pyridyl-1,2,3-triazole derivatives bearing a 4-amino-substituted benzenesulfonamide arm: synthesis, crystal structure, computational studies and inhibitory activity against carbonic anhydrase I, II, and IX isoforms† | Full Text | References | PDF (1.6 MB) | Supplemental
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Article
Osteopontin – a biomarker of disease, but also of stage stratification of the functional myocardial contractile deficit by chronic ischaemic heart disease
Bogdan-Ioan Coculescu, Gheorghe Manole, Gabi Valeriu Dincă, Elena Claudia Coculescu, Cristina Berteanu & Cristina Mariana Stocheci
Pages: 783-788
Published online: 07 Mar 2019
AbstractforOsteopontin – a biomarker of disease, but also of stage stratification of the functional myocardial contractile deficit by chronic ischaemic heart disease | Full Text | References | PDF (1 MB) | EPUB
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Article
The protective role of jervine against radiation-induced gastrointestinal toxicity
Selvinaz Yakan, Tuba Aydin, Canan Gulmez, Ozkan Ozden, Kivilcim Eren Erdogan, Yusuf Kenan Daglioglu, Fundagul Andic, Onur Atakisi & Ahmet Cakir
Pages: 789-798
Published online: 14 Mar 2019
AbstractforThe protective role of jervine against radiation-induced gastrointestinal toxicity | Full Text | References | PDF (2.3 MB) | EPUB
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Article
CRISPR/Cas9-based liver-derived reporter cells for screening of mPGES-1 inhibitors
Zhanfei Chen, Xiaoling Cai, Man Li, LinLin Yan, Luxi Wu, Xiaoqian Wang & Nanhong Tang
Pages: 799-807
Published online: 18 Mar 2019
AbstractforCRISPR/Cas9-based liver-derived reporter cells for screening of mPGES-1 inhibitors | Full Text | References | PDF (1.3 MB) | EPUB
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Article
Discovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping
Zhimin Zhang, Lili Gu, Beibei Wang, Wenhai Huang, Yanmin Zhang, Zhen Ma, Shenxin Zeng & Zhengrong Shen
Pages: 808-817
Published online: 18 Mar 2019
AbstractforDiscovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping | Full Text | References | PDF (2 MB) | EPUB
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Article
The antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitor
Qian Yu, Yu Chen, Hui Yang, Hong-Li Zhang, Keli Agama, Yves Pommier & Lin-Kun An
Pages: 818-822
Published online: 25 Mar 2019
AbstractforThe antitumor activity of CYB-L10, a human topoisomerase IB catalytic inhibitor | Full Text | References | PDF (699 KB) | EPUB | Supplemental
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New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents
Laurent R. Chiarelli, Matteo Mori, Giangiacomo Beretta, Arianna Gelain, Elena Pini, Josè Camilla Sammartino, Giovanni Stelitano, Daniela Barlocco, Luca Costantino, Margherita Lapillo, Giulio Poli, Isabella Caligiuri, Flavio Rizzolio, Marco Bellinzoni, Tiziano Tuccinardi, Stefania Villa & Fiorella Meneghetti
Pages: 823-828
Published online: 20 Mar 2019
AbstractforNew insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Article
Design, synthesis, and apoptosis-promoting effect evaluation of novel pyrazole with benzo[d]thiazole derivatives containing aminoguanidine units
Da Chuan Liu, Mei Jia Gao, Qiang Huo, Tao Ma, Ying Wang & Cheng Zhu Wu
Pages: 829-837
Published online: 27 Mar 2019
AbstractforDesign, synthesis, and apoptosis-promoting effect evaluation of novel pyrazole with benzo[d]thiazole derivatives containing aminoguanidine units | Full Text | References | PDF (1.3 MB) | EPUB
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Article
Novel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profile
Aml E.-S. Mghwary, Ehab M. Gedawy, Aliaa M. Kamal & Suzan M. Abuel-Maaty
Pages: 838-852
Published online: 28 Mar 2019
AbstractforNovel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profile | Full Text | References | PDF (2 MB) | EPUB | Supplemental
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Article
Sesquiterpenoids and 2-(2-phenylethyl)chromones respectively acting as α-glucosidase and tyrosinase inhibitors from agarwood of an Aquilaria plant
Li Yang, Yi-Ling Yang, Wen-Hua Dong, Wei Li, Pei Wang, Xue Cao, Jing-Zhe Yuan, Hui-Qin Chen, Wen-Li Mei & Hao-Fu Dai
Pages: 853-862
Published online: 22 Apr 2019
AbstractforSesquiterpenoids and 2-(2-phenylethyl)chromones respectively acting as α-glucosidase and tyrosinase inhibitors from agarwood of an Aquilaria plant | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
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Article
SAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogs
Raed Shalaby, Jacobus P. Petzer, Anél Petzer, Usman M. Ashraf, Ealla Atari, Fawaz Alasmari, Sivarajan Kumarasamy, Youssef Sari & Ashraf Khalil
Pages: 863-876
Published online: 27 Mar 2019
AbstractforSAR and molecular mechanism studies of monoamine oxidase inhibition by selected chalcone analogs | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Article
In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Jana Janockova, Jan Korabecny, Jana Plsikova, Katerina Babkova, Eva Konkolova, Dana Kucerova, Jana Vargova, Jan Koval, Rastislav Jendzelovsky, Peter Fedorocko, Jana Kasparkova, Viktor Brabec, Jan Rosocha, Ondrej Soukup, Slavka Hamulakova, Kamil Kuca & Maria Kozurkova
Pages: 877-897
Published online: 02 Apr 2019
AbstractforIn vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Antioxidant activity and antibacterial evaluation of new thiazolin-4-one derivatives as potential tryptophanyl-tRNA synthetase inhibitors
Anca Stana, Dan C. Vodnar, Gabriel Marc, Daniela Benedec, Brînduşa Tiperciuc, Radu Tamaian & Ovidiu Oniga
Pages: 898-908
Published online: 02 Apr 2019
AbstractforAntioxidant activity and antibacterial evaluation of new thiazolin-4-one derivatives as potential tryptophanyl-tRNA synthetase inhibitors | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 2016 Views
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Article
Design, synthesis and molecular mechanisms of novel dual inhibitors of heat shock protein 90/phosphoinositide 3-kinase alpha (Hsp90/PI3Kα) against cutaneous melanoma
Feifei Qin, Yali Wang, Xian Jiang, Yujia Wang, Nan Zhang, Xiang Wen, Lian Wang, Qinglin Jiang & Gu He
Pages: 909-926
Published online: 07 Apr 2019
AbstractforDesign, synthesis and molecular mechanisms of novel dual inhibitors of heat shock protein 90/phosphoinositide 3-kinase alpha (Hsp90/PI3Kα) against cutaneous melanoma | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Evaluation of caffeine as inhibitor against collagenase, elastase and tyrosinase using in silico and in vitro approach
Kyung Eun Lee, Shiv Bharadwaj, Umesh Yadava & Sang Gu Kang
Pages: 927-936
Published online: 30 Apr 2019
AbstractforEvaluation of caffeine as inhibitor against collagenase, elastase and tyrosinase using in silico and in vitro approach | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
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Article

Article
Benzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism
Wen-Jia Dan, Qiang Zhang, Fan Zhang, Wei-Wei Wang & Jin-Ming Gao
Pages: 937-945
Published online: 09 May 2019
AbstractforBenzonate derivatives of acetophenone as potent α-glucosidase inhibitors: synthesis, structure–activity relationship and mechanism | Full Text | References | PDF (1.2 MB) | EPUB
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Article
Thermostability enhancement of the α-carbonic anhydrase from Sulfurihydrogenibium yellowstonense by using the anchoring-and-self-labelling-protein-tag system (ASLtag)
Sonia Del Prete, Rosa Merlo, Anna Valenti, Rosanna Mattossovich, Mosè Rossi, Vincenzo Carginale, Claudiu T. Supuran, Giuseppe Perugino & Clemente Capasso
Pages: 946-954
Published online: 30 Apr 2019
AbstractforThermostability enhancement of the α-carbonic anhydrase from Sulfurihydrogenibium yellowstonense by using the anchoring-and-self-labelling-protein-tag system (ASLtag) | Full Text | References | PDF (1.3 MB) | EPUB
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Research Paper

Article
Design, synthesis, and anticancer evaluation of novel quinoline derivatives of ursolic acid with hydrazide, oxadiazole, and thiadiazole moieties as potent MEK inhibitors
Xiao-Yan Jin, Hao Chen, Dong-Dong Li, A-Liang Li, Wen-Yan Wang & Wen Gu
Pages: 955-972
Published online: 09 May 2019
AbstractforDesign, synthesis, and anticancer evaluation of novel quinoline derivatives of ursolic acid with hydrazide, oxadiazole, and thiadiazole moieties as potent MEK inhibitors | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 4149 Views
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Article
Probing the role of an invariant active site His in family GH1 β-glycosidases
Andrea Strazzulli, Giuseppe Perugino, Marialuisa Mazzone, Mosè Rossi, Stephen G. Withers & Marco Moracci
Pages: 973-980
Published online: 10 May 2019
AbstractforProbing the role of an invariant active site His in family GH1 β-glycosidases | Full Text | References | PDF (1.3 MB) | EPUB
  • 1198 Views
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Article
Design, synthesis and biological activity evaluation of a new class of 2,4-thiazolidinedione compounds as insulin enhancers
Zou Huiying, Chen Guangying & Zhou Shiyang
Pages: 981-989
Published online: 10 May 2019
AbstractforDesign, synthesis and biological activity evaluation of a new class of 2,4-thiazolidinedione compounds as insulin enhancers | Full Text | References | PDF (1.2 MB) | EPUB
  • 3129 Views
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Article
Kinetic and computational molecular docking simulation study of novel kojic acid derivatives as anti-tyrosinase and antioxidant agents
Yan-Mei Chen, Chen Li, Wen-Jing Zhang, Yan Shi, Zi-Jie Wen, Qing-Xi Chen & Qin Wang
Pages: 990-998
Published online: 10 May 2019
AbstractforKinetic and computational molecular docking simulation study of novel kojic acid derivatives as anti-tyrosinase and antioxidant agents | Full Text | References | PDF (1.2 MB) | EPUB
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Article
A novel anti-platelet aggregation target of chinensinaphthol methyl ether and neojusticin B obtained from Rostellularia procumbens (L.) Nees
Songtao Wu, Yanfang Yang, Bo Liu, Zhoutao Xie, Weichen Xiong, Pengfei Hao, Wenping Xiao, Yuan Sun, Zhongzhu Ai & Hezhen Wu
Pages: 999-1009
Published online: 10 May 2019
AbstractforA novel anti-platelet aggregation target of chinensinaphthol methyl ether and neojusticin B obtained from Rostellularia procumbens (L.) Nees | Full Text | References | PDF (1.6 MB) | EPUB
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Article

Article
Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases
Martina Hrast, Kaja Rožman, Iza Ogris, Veronika Škedelj, Delphine Patin, Matej Sova, Hélène Barreteau, Stanislav Gobec, Simona Golič Grdadolnik & Anamarija Zega
Pages: 1010-1017
Published online: 10 May 2019
AbstractforEvaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Original Article

Article
Molecular modeling studies on the interactions of 7-methoxytacrine-4-pyridinealdoxime, 4-PA, 2-PAM, and obidoxime with VX-inhibited human acetylcholinesterase: a near attack conformation approach
Jorge Alberto Valle da Silva, Eugenie Nepovimova, Teodorico Castro Ramalho, Kamil Kuca & Tanos Celmar Costa França
Pages: 1018-1029
Published online: 10 May 2019
AbstractforMolecular modeling studies on the interactions of 7-methoxytacrine-4-pyridinealdoxime, 4-PA, 2-PAM, and obidoxime with VX-inhibited human acetylcholinesterase: a near attack conformation approach | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Research Paper

Article
Novel sulfonamide benzoquinazolinones as dual EGFR/HER2 inhibitors, apoptosis inducers and radiosensitizers
Aiten M. Soliman, Ali S. Alqahtani & Mostafa M. Ghorab
Pages: 1030-1040
Published online: 10 May 2019
AbstractforNovel sulfonamide benzoquinazolinones as dual EGFR/HER2 inhibitors, apoptosis inducers and radiosensitizers | Full Text | References | PDF (1.5 MB) | EPUB
  • 1637 Views
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Article
Impact of phytosterols on liver and distal colon metabolome in experimental murine colitis model: an explorative study
Nunzia Iaccarino, Jussara Amato, Bruno Pagano, Anna Di Porzio, Matteo Micucci, Luca Bolelli, Rita Aldini, Ettore Novellino, Roberta Budriesi & Antonio Randazzo
Pages: 1041-1050
Published online: 10 May 2019
AbstractforImpact of phytosterols on liver and distal colon metabolome in experimental murine colitis model: an explorative study | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1990 Views
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Article
Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies
Alessandra Ammazzalorso, Simone Carradori, Andrea Angeli, Atilla Akdemir, Barbara De Filippis, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Rosa Amoroso & Claudiu T. Supuran
Pages: 1051-1061
Published online: 10 May 2019
AbstractforFibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies | Full Text | References | PDF (1.8 MB)
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Original Article

Article
Structure-based design generated novel hydroxamic acid based preferential HDAC6 lead inhibitor with on-target cytotoxic activity against primary choroid plexus carcinoma
Shaymaa E. Kassab, Samar Mowafy, Aya M. Alserw, Joustin A. Seliem, Shahenda M. El-Naggar, Nesreen N. Omar & Mohamed M. Awad
Pages: 1062-1077
Published online: 09 May 2019
AbstractforStructure-based design generated novel hydroxamic acid based preferential HDAC6 lead inhibitor with on-target cytotoxic activity against primary choroid plexus carcinoma | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Research Paper

Article
Stereoselective pharmacokinetic and pharmacodynamic analysis of a CNS-active sulphamoylphenyl carbamate derivative
David Bibi, Bella Shusterman, Alessio Nocentini, Claudiu T. Supuran & Meir Bialer
Pages: 1078-1082
Published online: 24 May 2019
AbstractforStereoselective pharmacokinetic and pharmacodynamic analysis of a CNS-active sulphamoylphenyl carbamate derivative | Full Text | References | PDF (786.9 KB)
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Article
Synthesis and biological evaluation of 3–(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer’s disease agents
Yu-Heng Hu, Jie Yang, Yun Zhang, Ke-Chun Liu, Teng Liu, Jie Sun & Xiao-Jing Wang
Pages: 1083-1092
Published online: 22 May 2019
AbstractforSynthesis and biological evaluation of 3–(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer’s disease agents | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 2839 Views
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Short Communication

Rapid Communication
Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells
Mariana Bastos dos Santos, Daiane Bertholin Anselmo, Jéssica Gisleine de Oliveira, Bruna V. Jardim-Perassi, Diego Alves Monteiro, Gabriel Silva, Eleni Gomes, Ana Lucia Fachin, Mozart Marins, Débora Aparecida Pires de Campos Zuccari & Luis Octavio Regasini
Pages: 1093-1099
Published online: 23 May 2019
AbstractforAntiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells | Full Text | References | PDF (809.4 KB) | EPUB | Supplemental
  • 3065 Views
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Research Paper

Article
Leishmania infantum arginase: biochemical characterization and inhibition by naturally occurring phenolic substances
Andreza R. Garcia, Danielle M. P. Oliveira, Ana Claudia F. Amaral, Jéssica B. Jesus, Ana Carolina Rennó Sodero, Alessandra M. T. Souza, Claudiu T. Supuran, Alane B. Vermelho, Igor A. Rodrigues & Anderson S. Pinheiro
Pages: 1100-1109
Published online: 24 May 2019
AbstractforLeishmania infantum arginase: biochemical characterization and inhibition by naturally occurring phenolic substances | Full Text | References | PDF (1.8 MB) | Supplemental
  • 2777 Views
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Article
Design, synthesis, molecular modelling, and biological evaluation of novel substituted pyrimidine derivatives as potential anticancer agents for hepatocellular carcinoma
Naglaa Mohamed Ahmed, Mahmoud Youns, Moustafa Khames Soltan & Ahmed Mohammed Said
Pages: 1110-1120
Published online: 23 May 2019
AbstractforDesign, synthesis, molecular modelling, and biological evaluation of novel substituted pyrimidine derivatives as potential anticancer agents for hepatocellular carcinoma | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
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Short Communication

Rapid Communication
Design and synthesis of novel pyrazolo[4,3-d]pyrimidines as potential therapeutic agents for acute lung injury
Bao Shi Wang, Xin Huang, Liu Zeng Chen, Ming Ming Liu & Jing Bo Shi
Pages: 1121-1130
Published online: 23 May 2019
AbstractforDesign and synthesis of novel pyrazolo[4,3-d]pyrimidines as potential therapeutic agents for acute lung injury | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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Original Articles

Article
Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis
Veronica Di Paolo, Chiara Fulci, Dante Rotili, Francesca Sciarretta, Alessia Lucidi, Blasco Morozzo della Rocca, Anastasia De Luca, Antonio Rosato, Luigi Quintieri & Anna Maria Caccuri
Pages: 1131-1139
Published online: 06 Jun 2019
AbstractforSynthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis | Full Text | References | PDF (1.5 MB) | EPUB
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Article
Discovery and antitumor evaluation of novel inhibitors of spermine oxidase
Lidan Sun, Jianlin Yang, Yu Qin, Yanlin Wang, Hongyan Wu, You Zhou & Chunyu Cao
Pages: 1140-1151
Published online: 03 Jun 2019
AbstractforDiscovery and antitumor evaluation of novel inhibitors of spermine oxidase | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
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Short Communication

Rapid Communication
Identification of novel indole derivatives acting as inhibitors of the Keap1–Nrf2 interaction
Barbara Cosimelli, Giovanni Greco, Sonia Laneri, Ettore Novellino, Antonia Sacchi, Giorgio Amendola, Sandro Cosconati, Roberta Bortolozzi & Giampietro Viola
Pages: 1152-1157
Published online: 09 Jun 2019
AbstractforIdentification of novel indole derivatives acting as inhibitors of the Keap1–Nrf2 interaction | Full Text | References | PDF (999.4 KB) | EPUB | Supplemental
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Short Communications

Rapid Communication
Identification of phenazine analogue as a novel scaffold for thioredoxin reductase I inhibitors against Hep G2 cancer cell lines
Jianming Liao, Linlin Wang, Zhongxi Wu, Zhixiang Wang, Jun Chen, Yucheng Zhong, Feng Jiang & Yuanyuan Lu
Pages: 1158-1163
Published online: 09 Jun 2019
AbstractforIdentification of phenazine analogue as a novel scaffold for thioredoxin reductase I inhibitors against Hep G2 cancer cell lines | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Research Paper

Article
Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani
Alessio Nocentini, Sameh M. Osman, Igor A. Rodrigues, Veronica S. Cardoso, Fatmah Ali S. Alasmary, Zeid AlOthman, Alane B. Vermelho, Paola Gratteri & Claudiu T. Supuran
Pages: 1164-1171
Published online: 20 Jun 2019
AbstractforAppraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani | Full Text | References | PDF (1.4 MB)
  • 1452 Views
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Article
Synthesis and biological evaluation of novel 8-substituted quinoline-2-carboxamides as carbonic anhydrase inhibitors
Pavitra S. Thacker, Pirpasha Shaikh, Andrea Angeli, Mohammed Arifuddin & Claudiu T. Supuran
Pages: 1172-1177
Published online: 20 Jun 2019
AbstractforSynthesis and biological evaluation of novel 8-substituted quinoline-2-carboxamides as carbonic anhydrase inhibitors | Full Text | References | PDF (994 KB) | Supplemental
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Article
The first activation study of the β-carbonic anhydrases from the pathogenic bacteria Brucella suis and Francisella tularensis with amines and amino acids
Andrea Angeli, Sonia Del Prete, Mariana Pinteala, Stelian S. Maier, William A. Donald, Bogdan C. Simionescu, Clemente Capasso & Claudiu T. Supuran
Pages: 1178-1185
Published online: 08 Jul 2019
AbstractforThe first activation study of the β-carbonic anhydrases from the pathogenic bacteria Brucella suis and Francisella tularensis with amines and amino acids | Full Text | References | PDF (1.2 MB)
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Article
Seeking new approach for therapeutic treatment of cholera disease via inhibition of bacterial carbonic anhydrases: experimental and theoretical studies for sixteen benzenesulfonamide derivatives
Rosaria Gitto, Laura De Luca, Francesca Mancuso, Sonia Del Prete, Daniela Vullo, Claudiu T. Supuran & Clemente Capasso
Pages: 1186-1192
Published online: 08 Jul 2019
AbstractforSeeking new approach for therapeutic treatment of cholera disease via inhibition of bacterial carbonic anhydrases: experimental and theoretical studies for sixteen benzenesulfonamide derivatives | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Original Article

Article
Activation of human α-carbonic anhydrase isoforms I, II, IV and VII with bis-histamine schiff bases and bis-spinaceamine substituted derivatives
Suleyman Akocak, Nabih Lolak, Silvia Bua, Alessio Nocentini & Claudiu T. Supuran
Pages: 1193-1198
Published online: 25 Jun 2019
AbstractforActivation of human α-carbonic anhydrase isoforms I, II, IV and VII with bis-histamine schiff bases and bis-spinaceamine substituted derivatives | Full Text | References | PDF (800.6 KB)
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Research Paper

Article
Synthesis of a new series of 3-functionalised-1-phenyl-1,2,3-triazole sulfamoylbenzamides as carbonic anhydrase I, II, IV and IX inhibitors
Baijayantimala Swain, Andrea Angeli, Srinivas Angapelly, Pavitra S. Thacker, Priti Singh, Claudiu T. Supuran & Mohammed Arifuddin
Pages: 1199-1209
Published online: 25 Jun 2019
AbstractforSynthesis of a new series of 3-functionalised-1-phenyl-1,2,3-triazole sulfamoylbenzamides as carbonic anhydrase I, II, IV and IX inhibitors | Full Text | References | PDF (1.5 MB)
  • 1911 Views
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Article
Synthesis, activity evaluation, and pro-apoptotic properties of novel 1,2,4-triazol-3-amine derivatives as potent anti-lung cancer agents
Xian-yu Sun, Chun-yan Zhong, Qing-qing Qiu, Zhen-wang Li, Mei-yu Liu, Xin Wang & Cheng-hao Jin
Pages: 1210-1217
Published online: 09 Jul 2019
AbstractforSynthesis, activity evaluation, and pro-apoptotic properties of novel 1,2,4-triazol-3-amine derivatives as potent anti-lung cancer agents | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1400 Views
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Article
1D NMR WaterLOGSY as an efficient method for fragment-based lead discovery
Claire Raingeval, Olivier Cala, Béatrice Brion, Marc Le Borgne, Roderick Eliot Hubbard & Isabelle Krimm
Pages: 1218-1225
Published online: 09 Jul 2019
Abstractfor1D NMR WaterLOGSY as an efficient method for fragment-based lead discovery | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
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Review Article

Review
Synthesis, antiasthmatic, and insecticidal/antifungal activities of allosamidins
Gangliang Huang & Hualiang Huang
Pages: 1226-1232
Published online: 16 Jul 2019
AbstractforSynthesis, antiasthmatic, and insecticidal/antifungal activities of allosamidins | Full Text | References | PDF (922 KB) | EPUB
  • 1385 Views
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Research Paper

Article
Discovery of aminopyridine-containing spiro derivatives as EGFR mutations inhibitors
Lianbao Ye, Tao Zhao, Wenjun Du, Anhu Li, Wei Gao, Jingrong Li, Ling Wang & Weiqiang Chen
Pages: 1233-1246
Published online: 09 Jul 2019
AbstractforDiscovery of aminopyridine-containing spiro derivatives as EGFR mutations inhibitors | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
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Article
In vitro anticancer potentiality and molecular modelling study of novel amino acid derivatives based on N1,N3-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamide
Asmaa F. Kassem, Gaber O. Moustafa, Eman S. Nossier, Hemat S. Khalaf, Marwa M. Mounier, Suliman A. Al-Yousef & Sabry Y. Mahmoud
Pages: 1247-1258
Published online: 09 Jul 2019
AbstractforIn vitro anticancer potentiality and molecular modelling study of novel amino acid derivatives based on N1,N3-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamide | Full Text | References | PDF (1.3 MB) | EPUB
  • 1400 Views
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Article
Novel phthalimide based analogues: design, synthesis, biological evaluation, and molecular docking studies
Ismail M. M. Othman, Mohamed A. M. Gad-Elkareem, Mohamed El-Naggar, Eman S. Nossier & Abd El-Galil E. Amr
Pages: 1259-1270
Published online: 09 Jul 2019
AbstractforNovel phthalimide based analogues: design, synthesis, biological evaluation, and molecular docking studies | Full Text | References | PDF (1.5 MB) | EPUB
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Article
Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1
Bianka Edina Herman, Anita Kiss, János Wölfling, Erzsébet Mernyák, Mihály Szécsi & Gyula Schneider
Pages: 1271-1286
Published online: 16 Jul 2019
AbstractforSynthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1 | Full Text | References | PDF (1.6 MB)
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Original Article

Article
Potential multifunctional agents with anti-hepatoma and anti-inflammation properties by inhibiting NF-кB activation
Chang-Ming Su, Gui-Ge Hou, Chun-Hua Wang, Hong-Qin Zhang, Cheng Yang, Mei Liu & Yun Hou
Pages: 1287-1297
Published online: 10 Jul 2019
AbstractforPotential multifunctional agents with anti-hepatoma and anti-inflammation properties by inhibiting NF-кB activation | Full Text | References | PDF (2 MB) | EPUB | Supplemental
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Research Paper

Article
10H-1,9-diazaphenothiazine and its 10-derivatives: synthesis, characterisation and biological evaluation as potential anticancer agents
Beata Morak-Młodawska, Krystian Pluta, Małgorzata Latocha, Małgorzata Jeleń, Dariusz Kuśmierz, Kinga Suwińska, Aleksander Shkurenko, Zenon Czuba & Magdalena Jurzak
Pages: 1298-1306
Published online: 16 Jul 2019
Abstractfor10H-1,9-diazaphenothiazine and its 10-derivatives: synthesis, characterisation and biological evaluation as potential anticancer agents | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
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Short Communication

Rapid Communication
Non-covalent immunoproteasome inhibitors induce cell cycle arrest in multiple myeloma MM.1R cells
Roberta Ettari, Giovanni Pallio, Gabriele Pizzino, Natasha Irrera, Maria Zappalà, Santina Maiorana, Carla Di Chio, Domenica Altavilla, Francesco Squadrito & Alessandra Bitto
Pages: 1307-1313
Published online: 16 Jul 2019
AbstractforNon-covalent immunoproteasome inhibitors induce cell cycle arrest in multiple myeloma MM.1R cells | Full Text | References | PDF (1.1 MB) | EPUB
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Rapid Communication
Computer-aided design and synthesis of 3-carbonyl-5-phenyl-1H-pyrazole as highly selective and potent BRAFV600E and CRAF inhibitor
Jinwoong Kim, Byeongha Choi, Daseul Im, Hoyong Jung, Hyungwoo Moon, Waqar Aman & Jung-Mi Hah
Pages: 1314-1320
Published online: 16 Jul 2019
AbstractforComputer-aided design and synthesis of 3-carbonyl-5-phenyl-1H-pyrazole as highly selective and potent BRAFV600E and CRAF inhibitor | Full Text | References | PDF (1.1 MB) | EPUB
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Review Article

Review
Carbazole scaffolds in cancer therapy: a review from 2012 to 2018
Samar Issa, Anthony Prandina, Nicolas Bedel, Pål Rongved, Saïd Yous, Marc Le Borgne & Zouhair Bouaziz
Pages: 1321-1346
Published online: 22 Jul 2019
AbstractforCarbazole scaffolds in cancer therapy: a review from 2012 to 2018 | Full Text | References | PDF (6.3 MB)
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Original Article

Article
Design and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibition
Salwa Elmeligie, Asmaa M. Aboul-Magd, Deena S. Lasheen, Tamer M. Ibrahim, Tamer M. Abdelghany, Sohair M. Khojah & Khaled A. M. Abouzid
Pages: 1347-1367
Published online: 19 Jul 2019
AbstractforDesign and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibition | Full Text | References | PDF (3 MB) | EPUB | Supplemental
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Short Communication

Rapid Communication
Novel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity
Xin Hao, Gang Qi, Hongxing Ma, Changjin Zhu & Zhongfei Han
Pages: 1368-1372
Published online: 26 Jul 2019
AbstractforNovel 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives as potent and selective aldose reductase inhibitors with antioxidant activity | Full Text | References | PDF (897.7 KB) | EPUB | Supplemental
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Research Paper

Article
Discovery of new butyrylcholinesterase inhibitors via structure-based virtual screening
Noor Atatreh, Sara Al Rawashdah, Shaikha S. Al Neyadi, Sawsan M. Abuhamdah & Mohammad A. Ghattas
Pages: 1373-1379
Published online: 26 Jul 2019
AbstractforDiscovery of new butyrylcholinesterase inhibitors via structure-based virtual screening | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
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Article
Anticancer sulfonamide hybrids that inhibit bladder cancer cells growth and migration as tubulin polymerisation inhibitors
Jia Liu, Chunlai Liu, Xiling Zhang, Liu Yu, Xue Gong & Ping Wang
Pages: 1380-1387
Published online: 11 Aug 2019
AbstractforAnticancer sulfonamide hybrids that inhibit bladder cancer cells growth and migration as tubulin polymerisation inhibitors | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
  • 1687 Views
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Article
New peptide derived antimalaria and antimicrobial agents bearing sulphonamide moiety
D. I. Ugwuja, U. C. Okoro, S. S. Soman, R. Soni, S. N. Okafor & D. I. Ugwu
Pages: 1388-1399
Published online: 08 Aug 2019
AbstractforNew peptide derived antimalaria and antimicrobial agents bearing sulphonamide moiety | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1666 Views
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Article
Design, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold
Giulia Rotondi, Paolo Guglielmi, Simone Carradori, Daniela Secci, Celeste De Monte, Barbara De Filippis, Cristina Maccallini, Rosa Amoroso, Roberto Cirilli, Atilla Akdemir, Andrea Angeli & Claudiu T. Supuran
Pages: 1400-1413
Published online: 11 Aug 2019
AbstractforDesign, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold | Full Text | References | PDF (3.7 MB)
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Original Article

Article
Synthesis and enzyme-based evaluation of analogues L-tyrosine thiol carboxylic acid inhibitor of metallo-β-lactamase IMP-1
Omid Khalili Arjomandi, Mahboubeh Kavoosi & Hadi Adibi
Pages: 1414-1425
Published online: 11 Aug 2019
AbstractforSynthesis and enzyme-based evaluation of analogues L-tyrosine thiol carboxylic acid inhibitor of metallo-β-lactamase IMP-1 | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1648 Views
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Research Paper

Article
Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors
Yunju Nam, Dongkeun Hwang, Namdoo Kim, Hong-Seog Seo, Khalid B. Selim & Taebo Sim
Pages: 1426-1438
Published online: 11 Aug 2019
AbstractforIdentification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors | Full Text | References | PDF (1.4 MB) | EPUB
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Article
Dual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) from Leishmania chagasi
Bárbara Velame Ferreira Teixeira, André Lacerda Braga Teles, Suellen Gonçalves da Silva, Camila Carane Bitencourt Brito, Humberto Fonseca de Freitas, Acássia Benjamim Leal Pires, Thamires Quadros Froes & Marcelo Santos Castilho
Pages: 1439-1450
Published online: 14 Aug 2019
AbstractforDual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) from Leishmania chagasi | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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Article
Kinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D↑G↑S mutant in the South African HIV-1 subtype C protease
Sibusiso Maseko, Eden Padayachee, Siyabonga Maphumulo, Thavendran Govender, Yasien Sayed, Glenn Maguire, Johnson Lin, Tricia Naicker, Sooraj Baijnath & Kruger Hendrik Gerhardus
Pages: 1451-1456
Published online: 14 Aug 2019
AbstractforKinetic and thermodynamic characterisation of HIV-protease inhibitors against E35D↑G↑S mutant in the South African HIV-1 subtype C protease | Full Text | References | PDF (1,007.1 KB) | EPUB | Supplemental
  • 1864 Views
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Article
Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamides as carbonic anhydrase isoforms I and II inhibitors
Mohammad M. Al-Sanea, Ahmed Elkamhawy, Sora Paik, Silvia Bua, So Ha Lee, Mohamed A. Abdelgawad, Eun Joo Roh, Wagdy M. Eldehna & Claudiu T. Supuran
Pages: 1457-1464
Published online: 14 Aug 2019
AbstractforSynthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamides as carbonic anhydrase isoforms I and II inhibitors | Full Text | References | PDF (1.1 MB)
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Article
Design, synthesis and biological evaluation of N-substituted α-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activity
Laureano L. Sabatier, Pablo H. Palestro, Andrea V. Enrique, Valentina Pastore, María L. Sbaraglini, Pedro Martín & Luciana Gavernet
Pages: 1465-1473
Published online: 14 Aug 2019
AbstractforDesign, synthesis and biological evaluation of N-substituted α-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activity | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 1307 Views
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Article
A fast, miniaturised in-vitro assay developed for quantification of lipase enzyme activity
Ariane Menden, Davane Hall, Daniel Paris, Venkatarian Mathura, Fiona Crawford, Michael Mullan, Stefan Crynen & Ghania Ait-Ghezala
Pages: 1474-1480
Published online: 15 Aug 2019
AbstractforA fast, miniaturised in-vitro assay developed for quantification of lipase enzyme activity | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
  • 2919 Views
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Article
Inhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity
Mincheol Kwon, Sung-Kyun Ko, Mina Jang, Gun-Hee Kim, In-Ja Ryoo, Sangkeun Son, Hyung Won Ryu, Sei-Ryang Oh, Won-Kyu Lee, Bo Yeon Kim, Jae-Hyuk Jang & Jong Seog Ahn
Pages: 1481-1488
Published online: 18 Aug 2019
AbstractforInhibitory effects of flavonoids isolated from Sophora flavescens on indoleamine 2,3-dioxygenase 1 activity | Full Text | References | PDF (1.4 MB) | EPUB
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Short Communication

Rapid Communication
Dual-target anti-Alzheimer’s disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activity
Zhisheng Mi, Bing Gan, Sihang Yu, Jianan Guo, Changjun Zhang, Xiaoying Jiang, Tao Zhou, Jing Su, Renren Bai & Yuanyuan Xie
Pages: 1489-1497
Published online: 16 Aug 2019
AbstractforDual-target anti-Alzheimer’s disease agents with both iron ion chelating and monoamine oxidase-B inhibitory activity | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
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Research Paper

Article
Exploring benzoxaborole derivatives as carbonic anhydrase inhibitors: a structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivity
Emma Langella, Vincenzo Alterio, Katia D’Ambrosio, Roberta Cadoni, Jean-Yves Winum, Claudiu T. Supuran, Simona Maria Monti, Giuseppina De Simone & Anna Di Fiore
Pages: 1498-1505
Published online: 18 Aug 2019
AbstractforExploring benzoxaborole derivatives as carbonic anhydrase inhibitors: a structural and computational analysis reveals their conformational variability as a tool to increase enzyme selectivity | Full Text | References | PDF (1.7 MB) | EPUB
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Exploration of the residues modulating the catalytic features of human carbonic anhydrase XIII by a site-specific mutagenesis approach
Giuseppina De Simone, Anna Di Fiore, Emanuela Truppo, Emma Langella, Daniela Vullo, Claudiu T. Supuran & Simona Maria Monti
Pages: 1506-1510
Published online: 20 Aug 2019
AbstractforExploration of the residues modulating the catalytic features of human carbonic anhydrase XIII by a site-specific mutagenesis approach | Full Text | References | PDF (1.1 MB) | EPUB
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Research Paper

Article
Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity
Paolo Guglielmi, Daniela Secci, Anél Petzer, Donatella Bagetta, Paola Chimenti, Giulia Rotondi, Claudio Ferrante, Lucia Recinella, Sheila Leone, Stefano Alcaro, Gokhan Zengin, Jacobus P. Petzer, Francesco Ortuso & Simone Carradori
Pages: 1511-1525
Published online: 19 Aug 2019
AbstractforBenzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity | Full Text | References | PDF (2.1 MB)
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Article
Exploring new structural features of the 4-[(3-methyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzenesulphonamide scaffold for the inhibition of human carbonic anhydrases
Simona Distinto, Rita Meleddu, Francesco Ortuso, Filippo Cottiglia, Serenella Deplano, Lisa Sequeira, Claudia Melis, Benedetta Fois, Andrea Angeli, Clemente Capasso, Rossella Angius, Stefano Alcaro, Claudiu T. Supuran & Elias Maccioni
Pages: 1526-1533
Published online: 20 Aug 2019
AbstractforExploring new structural features of the 4-[(3-methyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzenesulphonamide scaffold for the inhibition of human carbonic anhydrases | Full Text | References | PDF (2 MB) | EPUB
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Article
Design, synthesis, in vitro potent antiproliferative activity, and kinase inhibitory effects of new triarylpyrazole derivatives possessing different heterocycle terminal moieties
Mahmoud M. Gamal El-Din, Mohammed I. El-Gamal, Mohammed S. Abdel-Maksoud, Kyung Ho Yoo & Chang-Hyun Oh
Pages: 1534-1543
Published online: 27 Aug 2019
AbstractforDesign, synthesis, in vitro potent antiproliferative activity, and kinase inhibitory effects of new triarylpyrazole derivatives possessing different heterocycle terminal moieties | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
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Article
Synthesis and biological evaluation of novel N-(piperazin-1-yl)alkyl-1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential MEK inhibitors
Hao Chen, Chao Qiao, Ting-Ting Miao, A-Liang Li, Wen-Yan Wang & Wen Gu
Pages: 1544-1561
Published online: 25 Aug 2019
AbstractforSynthesis and biological evaluation of novel N-(piperazin-1-yl)alkyl-1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential MEK inhibitors | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Research Article

Article
Synthesis, computational studies, tyrosinase inhibitory kinetics and antimelanogenic activity of hydroxy substituted 2-[(4-acetylphenyl)amino]-2-oxoethyl derivatives
Muhammad Rafiq, Yasir Nazir, Zaman Ashraf, Hummera Rafique, Samina Afzal, Amara Mumtaz, Mubashir Hassan, Anser Ali, Khurram Afzal, Muhammad Rizwan Yousuf, Muhammad Saleem, Katarzyna Kotwica-Mojzych & Mariusz Mojzych
Pages: 1562-1572
Published online: 28 Aug 2019
AbstractforSynthesis, computational studies, tyrosinase inhibitory kinetics and antimelanogenic activity of hydroxy substituted 2-[(4-acetylphenyl)amino]-2-oxoethyl derivatives | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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Article
Towards discovery of novel scaffold with potent antiangiogenic activity; design, synthesis of pyridazine based compounds, impact of hinge interaction, and accessibility of their bioactive conformation on VEGFR-2 activities
Maiy Y. Jaballah, Rabah A. T. Serya, Nasser Saad, Sohair M. Khojah, Marawan Ahmed, Khaled Barakat & Khaled A. M. Abouzid
Pages: 1573-1589
Published online: 06 Sep 2019
AbstractforTowards discovery of novel scaffold with potent antiangiogenic activity; design, synthesis of pyridazine based compounds, impact of hinge interaction, and accessibility of their bioactive conformation on VEGFR-2 activities | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
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Review
Design and application of oral colon administration system
Hao Cheng, Shiyu Huang & Gangliang Huang
Pages: 1590-1596
Published online: 03 Oct 2019
AbstractforDesign and application of oral colon administration system | Full Text | References | PDF (643.8 KB) | EPUB
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Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists
Kejing Lao, Guoliang Xun, Xingchun Gou & Hua Xiang
Pages: 1597-1606
Published online: 30 Aug 2019
AbstractforDesign, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
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Article
Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone
Shaoyong Ke, Zhigang Zhang, Manli Liu, Wei Fang, Daye Huang, Zhongyi Wan, Ronghua Zhou, Kaimei Wang & Liqiao Shi
Pages: 1607-1614
Published online: 02 Sep 2019
AbstractforSynthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone | Full Text | References | PDF (981.3 KB) | EPUB
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Review
An overview of carbonic anhydrases and membrane channels of synoviocytes in inflamed joints
Min Jeong Ji & Jeong Hee Hong
Pages: 1615-1622
Published online: 03 Sep 2019
AbstractforAn overview of carbonic anhydrases and membrane channels of synoviocytes in inflamed joints | Full Text | References | PDF (1.1 MB) | EPUB
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Article
Competitive α-glucosidase inhibitors, dihydrobenzoxanthones, from the barks of Artocarpus elasticus
Janar Jenis, Aizhamal Baiseitova, Sang Hwa Yoon, Chanin Park, Jeong Yoon Kim, Zuo Peng Li, Keun Woo Lee & Ki Hun Park
Pages: 1623-1632
Published online: 03 Sep 2019
AbstractforCompetitive α-glucosidase inhibitors, dihydrobenzoxanthones, from the barks of Artocarpus elasticus | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Article
Novel tyrosinase inhibitory peptide with free radical scavenging ability
Zhiwei Shen, Yujiao Wang, Zhen Guo, Tingyuan Tan & Yi Zhang
Pages: 1633-1640
Published online: 08 Sep 2019
AbstractforNovel tyrosinase inhibitory peptide with free radical scavenging ability | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 3715 Views
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Review
Exosomes in head and neck cancer. Updating and revisiting
Samuel Rodríguez Zorrilla, Abel García García, Andrés Blanco Carrión, Pilar Gándara Vila, Manuel Somoza Martín, Mercedes Gallas Torreira & Mario Pérez Sayans
Pages: 1641-1651
Published online: 08 Sep 2019
AbstractforExosomes in head and neck cancer. Updating and revisiting | Full Text | References | PDF (1.3 MB) | EPUB
  • 2409 Views
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Review
Activation of α-, β-, γ- δ-, ζ- and η- class of carbonic anhydrases with amines and amino acids: a review
Suleyman Akocak & Claudiu T. Supuran
Pages: 1652-1659
Published online: 17 Sep 2019
AbstractforActivation of α-, β-, γ- δ-, ζ- and η- class of carbonic anhydrases with amines and amino acids: a review | Full Text | References | PDF (834.8 KB) | EPUB
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Article
Anti-Helicobacter pylori activity of ethoxzolamide
Joyanta K. Modak, Alexandra Tikhomirova, Rebecca J. Gorrell, Mohammad M. Rahman, Despina Kotsanas, Tony M. Korman, Jose Garcia-Bustos, Terry Kwok, Richard L. Ferrero, Claudiu T. Supuran & Anna Roujeinikova
Pages: 1660-1667
Published online: 17 Sep 2019
AbstractforAnti-Helicobacter pylori activity of ethoxzolamide | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Article
Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor
Yaling Zhang, Li Chen, Xiabing Li, Li Gao, Yunxia Hao, Baolin Li & Yaping Yan
Pages: 1668-1677
Published online: 17 Sep 2019
AbstractforNovel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
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Synthesis and in vitro and in vivo anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivatives
Wei-Yun Guo, Liu-Zeng Chen, Bang-Nian Shen, Xin-Hua Liu, Guang-Ping Tai, Qing-Shan Li, Li Gao & Ban-Feng Ruan
Pages: 1678-1689
Published online: 17 Sep 2019
AbstractforSynthesis and in vitro and in vivo anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivatives | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1568 Views
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Review Article

Review
Extraction and derivatisation of active polysaccharides
Yang Liu & Gangliang Huang
Pages: 1690-1696
Published online: 20 Sep 2019
AbstractforExtraction and derivatisation of active polysaccharides | Full Text | References | PDF (731.6 KB) | EPUB
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Article
Novel 2-substituted-benzimidazole-6-sulfonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IX and XII and molecular docking studies
Ciro Milite, Giorgio Amendola, Alessio Nocentini, Silvia Bua, Alessandra Cipriano, Elisabetta Barresi, Alessandra Feoli, Ettore Novellino, Federico Da Settimo, Claudiu T. Supuran, Sabrina Castellano, Sandro Cosconati & Sabrina Taliani
Pages: 1697-1710
Published online: 20 Sep 2019
AbstractforNovel 2-substituted-benzimidazole-6-sulfonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IX and XII and molecular docking studies | Full Text | References | PDF (3.8 MB) | EPUB | Supplemental
  • 2376 Views
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Blocking the FKBP12 induced dendrimeric burst in aberrant aggregation of α-synuclein by using the ElteN378 synthetic inhibitor
Gabriella Caminati, Maria Raffaella Martina, Stefano Menichetti & Piero Procacci
Pages: 1711-1715
Published online: 24 Sep 2019
AbstractforBlocking the FKBP12 induced dendrimeric burst in aberrant aggregation of α-synuclein by using the ElteN378 synthetic inhibitor | Full Text | References | PDF (898.4 KB) | EPUB | Supplemental
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Conformational restriction of a type II FMS inhibitor leading to discovery of 5-methyl-N-(2-aryl-1H-benzo[d]imidazo-5-yl)isoxazole-4-carboxamide analogues as selective FLT3 inhibitors
Daseul Im, Hyungwoo Moon, Jingwoong Kim, Youri Oh, Miyoung Jang & Jung-Mi Hah
Pages: 1716-1721
Published online: 01 Oct 2019
AbstractforConformational restriction of a type II FMS inhibitor leading to discovery of 5-methyl-N-(2-aryl-1H-benzo[d]imidazo-5-yl)isoxazole-4-carboxamide analogues as selective FLT3 inhibitors | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1179 Views
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Original Article

Article
Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones
Sinan Bilginer, Halise Inci Gul, Feyza Sena Erdal, Hiroshi Sakagami, Serkan Levent, Ilhami Gulcin & Claudiu T. Supuran
Pages: 1722-1729
Published online: 02 Oct 2019
AbstractforSynthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones | Full Text | References | PDF (955.7 KB) | EPUB
  • 1449 Views
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Article
1-(Piperidin-3-yl)thymine amides as inhibitors of M. tuberculosis thymidylate kinase
Yanlin Jian, Martijn D. P. Risseeuw, Mathy Froeyen, Lijun Song, Davie Cappoen, Paul Cos, Hélène Munier-Lehmann & Serge van Calenbergh
Pages: 1730-1739
Published online: 11 Dec 2019
Abstractfor1-(Piperidin-3-yl)thymine amides as inhibitors of M. tuberculosis thymidylate kinase | Full Text | References | PDF (1.3 MB) | EPUB | Supplemental
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