Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 33, Issue 1 (2018)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 33, Issue 1 (2018)

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Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance
Tim Fischer, Abdulkarim Najjar, Frank Totzke, Christoph Schächtele, Wolfgang Sippl, Christoph Ritter & Andreas Hilgeroth
Pages: 1-8
Published online: 03 Nov 2017
AbstractforDiscovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance | Full Text | References | PDF (1.4 MB)
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Article
Diaryl ethers with carboxymethoxyphenacyl motif as potent HIV-1 reverse transcriptase inhibitors with improved solubility
Tomasz Frączek, Rafał Kamiński, Agnieszka Krakowiak, Evelien Naessens, Bruno Verhasselt & Piotr Paneth
Pages: 9-16
Published online: 03 Nov 2017
AbstractforDiaryl ethers with carboxymethoxyphenacyl motif as potent HIV-1 reverse transcriptase inhibitors with improved solubility | Full Text | References | PDF (1.8 MB) | Supplemental
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Article
Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
Nazar Trotsko, Agata Przekora, Justyna Zalewska, Grażyna Ginalska, Agata Paneth & Monika Wujec
Pages: 17-24
Published online: 03 Nov 2017
AbstractforSynthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives | Full Text | References | PDF (896.6 KB) | Supplemental
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Article
Comparison of the amine/amino acid activation profiles of the β- and γ-carbonic anhydrases from the pathogenic bacterium Burkholderia pseudomallei
Daniela Vullo, Sonia Del Prete, Sameh M. Osman, Fatmah A. S. Alasmary, Zeid AlOthman, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 25-30
Published online: 03 Nov 2017
AbstractforComparison of the amine/amino acid activation profiles of the β- and γ-carbonic anhydrases from the pathogenic bacterium Burkholderia pseudomallei | Full Text | References | PDF (691.9 KB)
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Article
Sulphonamide inhibition studies of the β-carbonic anhydrase from the bacterial pathogen Clostridium perfringens
Daniela Vullo, R. Siva Sai Kumar, Andrea Scozzafava, James G. Ferry & Claudiu T. Supuran
Pages: 31-36
Published online: 03 Nov 2017
AbstractforSulphonamide inhibition studies of the β-carbonic anhydrase from the bacterial pathogen Clostridium perfringens | Full Text | References | PDF (696.5 KB)
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Article
Design, synthesis, and pharmacological evaluation of 2-amino-5-nitrothiazole derived semicarbazones as dual inhibitors of monoamine oxidase and cholinesterase: effect of the size of aryl binding site
Rati K. P. Tripathi, Vishnu M. Sasi, Sukesh K. Gupta, Sairam Krishnamurthy & Senthil R. Ayyannan
Pages: 37-57
Published online: 03 Nov 2017
AbstractforDesign, synthesis, and pharmacological evaluation of 2-amino-5-nitrothiazole derived semicarbazones as dual inhibitors of monoamine oxidase and cholinesterase: effect of the size of aryl binding site | Full Text | References | PDF (3.6 MB)
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Short Communication

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Synthesis of new pyridothienopyrimidinone and pyridothienotriazolopyrimidine derivatives as pim-1 inhibitors
Hala B. El-Nassan, Bassem H. Naguib & Engy A. Beshay
Pages: 58-66
Published online: 21 Nov 2017
AbstractforSynthesis of new pyridothienopyrimidinone and pyridothienotriazolopyrimidine derivatives as pim-1 inhibitors | Full Text | References | PDF (937.9 KB) | Supplemental
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Article
Benzo[g]quinazolin-based scaffold derivatives as dual EGFR/HER2 inhibitors
Mostafa M. Ghorab, Mansour S. Alsaid, Aiten M. Soliman & Abdullah A. Al-Mishari
Pages: 67-73
Published online: 03 Nov 2017
AbstractforBenzo[g]quinazolin-based scaffold derivatives as dual EGFR/HER2 inhibitors | Full Text | References | PDF (879.5 KB)
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Article
Design, synthesis and biological activity of N4-phenylsubstituted-7H-pyrrolo[2,3-d]pyrimidin-4-amines as dual inhibitors of aurora kinase A and epidermal growth factor receptor kinase
Sonali Kurup, Bradley McAllister, Pavlina Liskova, Trusha Mistry, Anthony Fanizza, Dan Stanford, Jolanta Slawska, Ulrich Keller & Alexander Hoellein
Pages: 74-84
Published online: 08 Nov 2017
AbstractforDesign, synthesis and biological activity of N4-phenylsubstituted-7H-pyrrolo[2,3-d]pyrimidin-4-amines as dual inhibitors of aurora kinase A and epidermal growth factor receptor kinase | Full Text | References | PDF (2.6 MB) | Supplemental
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Article
Selectivity analyses of γ-benzylidene digoxin derivatives to different Na,K-ATPase α isoforms: a molecular docking approach
Marco T. C. Pessôa, Silmara L. G. Alves, Alex G. Taranto, José A. F. P. Villar, Gustavo Blanco & Leandro A. Barbosa
Pages: 85-97
Published online: 08 Nov 2017
AbstractforSelectivity analyses of γ-benzylidene digoxin derivatives to different Na,K-ATPase α isoforms: a molecular docking approach | Full Text | References | PDF (3.3 MB) | Supplemental
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Article
Synthesis, physiochemical property and antimicrobial activity of novel quaternary ammonium salts
Xianrui Xie, Wei Cong, Feng Zhao, Hongjuan Li, Wenyu Xin, Guige Hou & Chunhua Wang
Pages: 98-105
Published online: 17 Nov 2017
AbstractforSynthesis, physiochemical property and antimicrobial activity of novel quaternary ammonium salts | Full Text | References | PDF (1.6 MB) | Supplemental
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Short Communication

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Macrocarpal C isolated from Eucalyptus globulus inhibits dipeptidyl peptidase 4 in an aggregated form
Eisuke Kato, Kazuhiro Kawakami & Jun Kawabata
Pages: 106-109
Published online: 17 Nov 2017
AbstractforMacrocarpal C isolated from Eucalyptus globulus inhibits dipeptidyl peptidase 4 in an aggregated form | Full Text | References | PDF (718 KB) | Supplemental
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Rapid Communication
Structure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors
Xiao-hui Gao, Lin-bo Liu, Hao-ran Liu, Jing-jing Tang, Lu Kang, Hongnian Wu, Peiwu Cui & Jianye Yan
Pages: 110-114
Published online: 22 Nov 2017
AbstractforStructure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors | Full Text | References | PDF (1.3 MB) | Supplemental
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Article
Gualou Guizhi decoction reverses brain damage with cerebral ischemic stroke, multi-component directed multi-target to screen calcium-overload inhibitors using combination of molecular docking and protein–protein docking
Juan Hu, Wen-Sheng Pang, Jing Han, Kuan Zhang, Ji-Zhou Zhang & Li-Dian Chen
Pages: 115-125
Published online: 29 Nov 2017
AbstractforGualou Guizhi decoction reverses brain damage with cerebral ischemic stroke, multi-component directed multi-target to screen calcium-overload inhibitors using combination of molecular docking and protein–protein docking | Full Text | References | PDF (3.5 MB)
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Article
Synthesis and antitumor activity of novel 2, 3-didithiocarbamate substituted naphthoquinones as inhibitors of pyruvate kinase M2 isoform
Xianling Ning, Hailong Qi, Ridong Li, Yan Jin, Michael A. McNutt & Yuxin Yin
Pages: 126-129
Published online: 29 Nov 2017
AbstractforSynthesis and antitumor activity of novel 2, 3-didithiocarbamate substituted naphthoquinones as inhibitors of pyruvate kinase M2 isoform | Full Text | References | PDF (610.2 KB)
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Short Communication

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New pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity
Qin Li, Juping Zhang, Liu Zeng Chen, Jie Quan Wang, Hai Ping Zhou, Wen Jian Tang, Wei Xue & Xin Hua Liu
Pages: 130-138
Published online: 04 Dec 2017
AbstractforNew pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity | Full Text | References | PDF (1.6 MB) | Supplemental
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Article
Nanoemulsions of sulfonamide carbonic anhydrase inhibitors strongly inhibit the growth of Trypanosoma cruzi
Alane Beatriz Vermelho, Verônica da Silva Cardoso, Eduardo Ricci Junior, Elisabete Pereira dos Santos & Claudiu T. Supuran
Pages: 139-146
Published online: 01 Dec 2017
AbstractforNanoemulsions of sulfonamide carbonic anhydrase inhibitors strongly inhibit the growth of Trypanosoma cruzi | Full Text | References | PDF (2.2 MB)
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Short Communication

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Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
Abdul-Malek S. Altamimi, Ahmed M. Alafeefy, Agnese Balode, Igor Vozny, Aleksandrs Pustenko, Mohey Eldin El Shikh, Fatmah A. S. Alasmary, Sherif A. Abdel-Gawad & Raivis Žalubovskis
Pages: 147-150
Published online: 04 Dec 2017
AbstractforSymmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A | Full Text | References | PDF (851.8 KB) | Supplemental
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Rapid Communication
Crystal structure of the human carbonic anhydrase II adduct with 1-(4-sulfamoylphenyl-ethyl)-2,4,6-triphenylpyridinium perchlorate, a membrane-impermeant, isoform selective inhibitor
Vincenzo Alterio, Davide Esposito, Simona Maria Monti, Claudiu T. Supuran & Giuseppina De Simone
Pages: 151-157
Published online: 04 Dec 2017
AbstractforCrystal structure of the human carbonic anhydrase II adduct with 1-(4-sulfamoylphenyl-ethyl)-2,4,6-triphenylpyridinium perchlorate, a membrane-impermeant, isoform selective inhibitor | Full Text | References | PDF (1.6 MB)
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Article
New cyclopentaquinoline hybrids with multifunctional capacities for the treatment of Alzheimer’s disease
Kamila Czarnecka, Małgorzata Girek, Karolina Maciejewska, Robert Skibiński, Jakub Jończyk, Marek Bajda, Jacek Kabziński, Przemysław Sołowiej, Ireneusz Majsterek & Paweł Szymański
Pages: 158-170
Published online: 06 Dec 2017
AbstractforNew cyclopentaquinoline hybrids with multifunctional capacities for the treatment of Alzheimer’s disease | Full Text | References | PDF (2.5 MB)
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Article
Synthesis and preliminary structure-activity relationship study of 2-aryl-2H-pyrazolo[4,3-c]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors
Ivana Malvacio, Alberto Cuzzolin, Mattia Sturlese, D. Mariano A. Vera, E. Laura Moyano & Stefano Moro
Pages: 171-183
Published online: 06 Dec 2017
AbstractforSynthesis and preliminary structure-activity relationship study of 2-aryl-2H-pyrazolo[4,3-c]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors | Full Text | References | PDF (2.6 MB) | Supplemental
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Article
Haemolytic anaemia and hepatocitolysis associated with hypermagnesaemia by repeated exposures to copper–calcium fungicides
Constantin Bălăeţ, Bogdan Ioan Coculescu, Maria Bălăeţ, Gheorghe Manole & Gabi Valeriu Dincă
Pages: 184-189
Published online: 12 Dec 2017
AbstractforHaemolytic anaemia and hepatocitolysis associated with hypermagnesaemia by repeated exposures to copper–calcium fungicides | Full Text | References | PDF (1.1 MB)
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Article
Synthesis and characterisation of celastrol derivatives as potential anticancer agents
Hong-Jian Zhang, Guo-Rui Zhang, Hu-Ri Piao & Zhe-Shan Quan
Pages: 190-198
Published online: 12 Dec 2017
AbstractforSynthesis and characterisation of celastrol derivatives as potential anticancer agents | Full Text | References | PDF (1.4 MB)
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Article
Synthesis and biological evaluation of 2-styrylquinolines as antitumour agents and EGFR kinase inhibitors: molecular docking study
Magda A.-A. El-Sayed, Walaa M. El-Husseiny, Naglaa I. Abdel-Aziz, Adel S. El-Azab, Hatem A. Abuelizz & Alaa A.-M. Abdel-Aziz
Pages: 199-209
Published online: 18 Dec 2017
AbstractforSynthesis and biological evaluation of 2-styrylquinolines as antitumour agents and EGFR kinase inhibitors: molecular docking study | Full Text | References | PDF (2.7 MB)
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Article
Benzimidazole derivatives endowed with potent antileishmanial activity
Michele Tonelli, Elena Gabriele, Francesca Piazza, Nicoletta Basilico, Silvia Parapini, Bruno Tasso, Roberta Loddo, Fabio Sparatore & Anna Sparatore
Pages: 210-226
Published online: 13 Dec 2017
AbstractforBenzimidazole derivatives endowed with potent antileishmanial activity | Full Text | References | PDF (3 MB)
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Article
Activation studies of the α- and β-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae with amines and amino acids
Andrea Angeli, Sonia Del Prete, Sameh M. Osman, Fatmah A. S. Alasmary, Zeid AlOthman, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 227-233
Published online: 12 Dec 2017
AbstractforActivation studies of the α- and β-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae with amines and amino acids | Full Text | References | PDF (780.5 KB)
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Article
Plasmatic carbonic anhydrase IX as a diagnostic marker for clear cell renal cell carcinoma
Laura Lucarini, Lucia Magnelli, Nicola Schiavone, Alfonso Crisci, Alessio Innocenti, Luca Puccetti, Fabio Cianchi, Sara Peri, Claudiu T. Supuran, Laura Papucci & Emanuela Masini
Pages: 234-240
Published online: 18 Dec 2017
AbstractforPlasmatic carbonic anhydrase IX as a diagnostic marker for clear cell renal cell carcinoma | Full Text | References | PDF (1 MB)
  • 1870 Views
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Article
Discovery of antimicrobial compounds targeting bacterial type FAD synthetases
María Sebastián, Ernesto Anoz-Carbonell, Begoña Gracia, Pilar Cossio, José Antonio Aínsa, Isaías Lans & Milagros Medina
Pages: 241-254
Published online: 19 Dec 2017
AbstractforDiscovery of antimicrobial compounds targeting bacterial type FAD synthetases | Full Text | References | PDF (2.6 MB) | Supplemental
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Short Communication

Rapid Communication
Inhibition studies of Brucella suis β-carbonic anhydrases with a series of 4-substituted pyridine-3-sulphonamides
Simona Maria Monti, Angela Meccariello, Mariangela Ceruso, Krzysztof Szafrański, Jarosław Sławiński & Claudiu T. Supuran
Pages: 255-259
Published online: 22 Dec 2017
AbstractforInhibition studies of Brucella suis β-carbonic anhydrases with a series of 4-substituted pyridine-3-sulphonamides | Full Text | References | PDF (1.2 MB)
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Research Paper

Article
Discovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s disease
Chen Zhang, Qian Zhou, Xu-Nian Wu, Ya-Dan Huang, Jie Zhou, Zengwei Lai, Yinuo Wu & Hai-Bin Luo
Pages: 260-270
Published online: 22 Dec 2017
AbstractforDiscovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s disease | Full Text | References | PDF (2.4 MB) | Supplemental
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Article
Small molecule purine and pseudopurine derivatives: synthesis, cytostatic evaluations and investigation of growth inhibitory effect in non-small cell lung cancer A549
Andrea Bistrović, Petra Grbčić, Anja Harej, Mirela Sedić, Sandra Kraljević-Pavelić, Sanja Koštrun, Janez Plavec, Damjan Makuc & Silvana Raić-Malić
Pages: 271-285
Published online: 22 Dec 2017
AbstractforSmall molecule purine and pseudopurine derivatives: synthesis, cytostatic evaluations and investigation of growth inhibitory effect in non-small cell lung cancer A549 | Full Text | References | PDF (4.5 MB) | Supplemental
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Short Communication

Rapid Communication
Carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles
Alessio Nocentini, Roberta Cadoni, Pascal Dumy, Claudiu T. Supuran & Jean-Yves Winum
Pages: 286-289
Published online: 27 Dec 2017
AbstractforCarbonic anhydrases from Trypanosoma cruzi and Leishmania donovani chagasi are inhibited by benzoxaboroles | Full Text | References | PDF (453.9 KB)
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Research Paper

Article
Synthesis and bioevaluation of new tacrine-cinnamic acid hybrids as cholinesterase inhibitors against Alzheimer’s disease
Yao Chen, Jie Zhu, Jun Mo, Hongyu Yang, Xueyang Jiang, Hongzhi Lin, Kai Gu, Yuqiong Pei, Liang Wu, Renxiang Tan, Jing Hou, Jingyi Chen, Yang Lv, Yaoyao Bian & Haopeng Sun
Pages: 290-302
Published online: 27 Dec 2017
AbstractforSynthesis and bioevaluation of new tacrine-cinnamic acid hybrids as cholinesterase inhibitors against Alzheimer’s disease | Full Text | References | PDF (2.6 MB) | Supplemental
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Short Communication

Rapid Communication
Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators
Andrea Angeli, Niccolò Chiaramonte, Dina Manetti, Maria Novella Romanelli & Claudiu T. Supuran
Pages: 303-308
Published online: 27 Dec 2017
AbstractforInvestigation of piperazines as human carbonic anhydrase I, II, IV and VII activators | Full Text | References | PDF (935.5 KB)
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Research Paper

Article
One-pot three-component synthesis of novel spirooxindoles with potential cytotoxic activity against triple-negative breast cancer MDA-MB-231 cells
Wagdy M. Eldehna, Dina H. EL-Naggar, Ahmed R. Hamed, Hany S. Ibrahim, Hazem A. Ghabbour & Hatem A. Abdel-Aziz
Pages: 309-318
Published online: 28 Dec 2017
AbstractforOne-pot three-component synthesis of novel spirooxindoles with potential cytotoxic activity against triple-negative breast cancer MDA-MB-231 cells | Full Text | References | PDF (1.8 MB) | Supplemental
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Article
Bulge oligonucleotide as an inhibitory agent of bacterial topoisomerase I
Zhaoqi Yang, Tuoyu Jiang, Hanshi Zhong & Yu Kang
Pages: 319-323
Published online: 28 Dec 2017
AbstractforBulge oligonucleotide as an inhibitory agent of bacterial topoisomerase I | Full Text | References | PDF (1,003.8 KB) | Supplemental
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Article
Design and synthesis of novel oridonin analogues as potent anticancer agents
Qing-Kun Shen, Zheng-Ai Chen, Hong-Jian Zhang, Jia-Li Li, Chuan-Feng Liu, Guo-Hua Gong & Zhe-Shan Quan
Pages: 324-333
Published online: 05 Jan 2018
AbstractforDesign and synthesis of novel oridonin analogues as potent anticancer agents | Full Text | References | PDF (1.3 MB)
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Article
Biochemical characterisation of a Kunitz-type inhibitor from Tamarindus indica L. seeds and its efficacy in reducing plasma leptin in an experimental model of obesity
Amanda Fernandes de Medeiros, Izael de Sousa Costa, Fabiana Maria Coimbra de Carvalho, Sumika Kiyota, Beatriz Blenda Pinheiro de Souza, Daniel Nogoceke Sifuentes, Raphael Paschoal Serquiz, Bruna Leal Lima Maciel, Adriana Ferreira Uchôa, Elizeu Antunes dos Santos & Ana Heloneida de Araújo Morais
Pages: 334-348
Published online: 11 Jan 2018
AbstractforBiochemical characterisation of a Kunitz-type inhibitor from Tamarindus indica L. seeds and its efficacy in reducing plasma leptin in an experimental model of obesity | Full Text | References | PDF (3.9 MB)
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Article
Chemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61
Andrea Calcaterra, Valentina Iovine, Bruno Botta, Deborah Quaglio, Ilaria D’Acquarica, Alessia Ciogli, Antonia Iazzetti, Romina Alfonsi, Ludovica Lospinoso Severini, Paola Infante, Lucia Di Marcotullio, Mattia Mori & Francesca Ghirga
Pages: 349-358
Published online: 17 Jan 2018
AbstractforChemical, computational and functional insights into the chemical stability of the Hedgehog pathway inhibitor GANT61 | Full Text | References | PDF (2 MB) | Supplemental
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Article
Anion inhibition studies of a beta carbonic anhydrase from the malaria mosquito Anopheles gambiae
Daniela Vullo, Leo Syrjänen, Marianne Kuuslahti, Seppo Parkkila & Claudiu T. Supuran
Pages: 359-363
Published online: 11 Jan 2018
AbstractforAnion inhibition studies of a beta carbonic anhydrase from the malaria mosquito Anopheles gambiae | Full Text | References | PDF (514.1 KB)
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Short Communication

Rapid Communication
Activation studies with amines and amino acids of the β-carbonic anhydrase encoded by the Rv3273 gene from the pathogenic bacterium Mycobacterium tuberculosis
Andrea Angeli, Sonia Del Prete, Sameh M. Osman, Fatmah A. S. Alasmary, Zeid AlOthman, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 364-369
Published online: 11 Jan 2018
AbstractforActivation studies with amines and amino acids of the β-carbonic anhydrase encoded by the Rv3273 gene from the pathogenic bacterium Mycobacterium tuberculosis | Full Text | References | PDF (723.1 KB)
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Research Article

Article
Enhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles
Anthony Prandina, Lars Herfindal, Sylvie Radix, Pål Rongved, Stein O. Døskeland, Marc Le Borgne & Florent Perret
Pages: 370-375
Published online: 16 Jan 2018
AbstractforEnhancement of iodinin solubility by encapsulation into cyclodextrin nanoparticles | Full Text | References | PDF (1.6 MB) | Supplemental
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Research Paper

Article
Insights into biological activity of ureidoamides with primaquine and amino acid moieties
Josipa Vlainić, Ivan Kosalec, Kristina Pavić, Dimitra Hadjipavlou-Litina, Eleni Pontiki & Branka Zorc
Pages: 376-382
Published online: 24 Jan 2018
AbstractforInsights into biological activity of ureidoamides with primaquine and amino acid moieties | Full Text | References | PDF (788.1 KB) | Supplemental
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Erratum

Correction
Correction to: Zhang et al., Discovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s disease
Page: 383
Published online: 24 Jan 2018
CitationforCorrection to: Zhang et al., Discovery of novel PDE9A inhibitors with antioxidant activities for treatment of Alzheimer’s disease | Full Text | PDF (138.6 KB)
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Conjugation of phosphonoacetic acid to nucleobase promotes a mechanism-based inhibition
Algirdas Mikalkėnas, Bazilė Ravoitytė, Daiva Tauraitė, Elena Servienė, Rolandas Meškys & Saulius Serva
Pages: 384-389
Published online: 26 Jan 2018
AbstractforConjugation of phosphonoacetic acid to nucleobase promotes a mechanism-based inhibition | Full Text | References | PDF (1.2 MB) | Supplemental
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Rapid Communication
Sulfonamide inhibition studies of two β-carbonic anhydrases from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2
Daniela Vullo, Ronny Lehneck, Stefanie Pöggeler & Claudiu T. Supuran
Pages: 390-396
Published online: 24 Jan 2018
AbstractforSulfonamide inhibition studies of two β-carbonic anhydrases from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2 | Full Text | References | PDF (686 KB)
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Research Paper

Article
Synthesis, biological activity and molecular modelling studies of shikimic acid derivatives as inhibitors of the shikimate dehydrogenase enzyme of Escherichia coli
Dulce Catalina Díaz-Quiroz, César Salvador Cardona-Félix, José Luis Viveros-Ceballos, Miguel Angel Reyes-González, Franciso Bolívar, Mario Ordoñez & Adelfo Escalante
Pages: 397-404
Published online: 24 Jan 2018
AbstractforSynthesis, biological activity and molecular modelling studies of shikimic acid derivatives as inhibitors of the shikimate dehydrogenase enzyme of Escherichia coli | Full Text | References | PDF (1.3 MB) | Supplemental
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Article
Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies
David Izuchukwu Ugwu, Uchechukwu Christopher Okoro, Pius Onyeoziri Ukoha, Astha Gupta & Sunday N. Okafor
Pages: 405-415
Published online: 26 Jan 2018
AbstractforNovel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies | Full Text | References | PDF (1.8 MB) | Supplemental
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Article
Synthesis and biological evaluation of stilbene derivatives coupled to NO donors as potential antidiabetic agents
Bing Wang, Teng Liu, Zhongyu Wu, Lei Zhang, Jie Sun & Xiaojing Wang
Pages: 416-423
Published online: 29 Jan 2018
AbstractforSynthesis and biological evaluation of stilbene derivatives coupled to NO donors as potential antidiabetic agents | Full Text | References | PDF (1 MB) | Supplemental
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Article
Differential expression of snoRNAs in oral squamous cell carcinomas: new potential diagnostic markers
Cintia Chamorro-Petronacci, Mario Perez-Sayáns, Maria Elena Padín-Iruegas, Xabier Marichalar-Mendia, Mercedes Gallas-Torreira & Abel García García
Pages: 424-427
Published online: 26 Jan 2018
AbstractforDifferential expression of snoRNAs in oral squamous cell carcinomas: new potential diagnostic markers | Full Text | References | PDF (1 MB)
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Article
Gamma-glutamyltransferase, possible novel biomarker in colon diverticulosis: a case-control study
Constantin Bălăeţ, Bogdan Ioan Coculescu, Gheorghe Manole, Maria Bălăeţ & Gabi Valeriu Dincă
Pages: 428-432
Published online: 26 Jan 2018
AbstractforGamma-glutamyltransferase, possible novel biomarker in colon diverticulosis: a case-control study | Full Text | References | PDF (1.1 MB)
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Corrigendum

Correction
Correction to: Fischer et al., Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance
Page: 433
Published online: 02 Feb 2018
CitationforCorrection to: Fischer et al., Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance | Full Text | PDF (138.6 KB)
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Research Paper

Article
N-thioalkylcarbazoles derivatives as new anti-proliferative agents: synthesis, characterisation and molecular mechanism evaluation
Maria Stefania Sinicropi, Domenico Iacopetta, Camillo Rosano, Rosario Randino, Anna Caruso, Carmela Saturnino, Noemi Muià, Jessica Ceramella, Francesco Puoci, Manuela Rodriquez, Pasquale Longo & Maria Rosaria Plutino
Pages: 434-444
Published online: 31 Jan 2018
AbstractforN-thioalkylcarbazoles derivatives as new anti-proliferative agents: synthesis, characterisation and molecular mechanism evaluation | Full Text | References | PDF (2.2 MB)
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Article
Design and synthesis of naphthalimide group-bearing thioglycosides as novel β-N-acetylhexosaminidases inhibitors
Shengqiang Shen, Wei Chen, Lili Dong, Qing Yang, Huizhe Lu & Jianjun Zhang
Pages: 445-452
Published online: 02 Feb 2018
AbstractforDesign and synthesis of naphthalimide group-bearing thioglycosides as novel β-N-acetylhexosaminidases inhibitors | Full Text | References | PDF (1.6 MB) | Supplemental
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Review Article

Review
Recent developments on triazole nucleus in anticonvulsant compounds: a review
Ming-Xia Song & Xian-Qing Deng
Pages: 453-478
Published online: 31 Jan 2018
AbstractforRecent developments on triazole nucleus in anticonvulsant compounds: a review | Full Text | References | PDF (3.8 MB)
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Research Paper

Article
Tricyclic coumarin sulphonate derivatives with alkaline phosphatase inhibitory effects: in vitro and docking studies
Jamshed Iqbal, Mohammed I. El-Gamal, Syeda Abida Ejaz, Joanna Lecka, Jean Sévigny & Chang-Hyun Oh
Pages: 479-484
Published online: 02 Feb 2018
AbstractforTricyclic coumarin sulphonate derivatives with alkaline phosphatase inhibitory effects: in vitro and docking studies | Full Text | References | PDF (1.1 MB) | Supplemental
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Article
Carbon- versus sulphur-based zinc binding groups for carbonic anhydrase inhibitors?
Claudiu T. Supuran
Pages: 485-495
Published online: 02 Feb 2018
AbstractforCarbon- versus sulphur-based zinc binding groups for carbonic anhydrase inhibitors? | Full Text | References | PDF (1.3 MB)
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Article
Synthesis, pharmacology and molecular docking on multifunctional tacrine-ferulic acid hybrids as cholinesterase inhibitors against Alzheimer’s disease
Jie Zhu, Hongyu Yang, Yao Chen, Hongzhi Lin, Qi Li, Jun Mo, Yaoyao Bian, Yuqiong Pei & Haopeng Sun
Pages: 496-506
Published online: 06 Feb 2018
AbstractforSynthesis, pharmacology and molecular docking on multifunctional tacrine-ferulic acid hybrids as cholinesterase inhibitors against Alzheimer’s disease | Full Text | References | PDF (2.8 MB) | Supplemental
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Article
Synthesis, antitumour and antioxidant activities of novel α,β-unsaturated ketones and related heterocyclic analogues: EGFR inhibition and molecular modelling study
Walaa M. El-Husseiny, Magda A.-A. El-Sayed, Naglaa I. Abdel-Aziz, Adel S. El-Azab, Esam R. Ahmed & Alaa A.-M. Abdel-Aziz
Pages: 507-518
Published online: 19 Feb 2018
AbstractforSynthesis, antitumour and antioxidant activities of novel α,β-unsaturated ketones and related heterocyclic analogues: EGFR inhibition and molecular modelling study | Full Text | References | PDF (2.4 MB) | Supplemental
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Short Communication

Rapid Communication
Structure–activity relationship investigation of tertiary amine derivatives of cinnamic acid as acetylcholinesterase and butyrylcholinesterase inhibitors: compared with that of phenylpropionic acid, sorbic acid and hexanoic acid
Xiaohui Gao, Jingjing Tang, Haoran Liu, Linbo Liu, Lu Kang & Wen Chen
Pages: 519-524
Published online: 15 Feb 2018
AbstractforStructure–activity relationship investigation of tertiary amine derivatives of cinnamic acid as acetylcholinesterase and butyrylcholinesterase inhibitors: compared with that of phenylpropionic acid, sorbic acid and hexanoic acid | Full Text | References | PDF (1 MB) | Supplemental
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Research Paper

Article
The discovery of novel HDAC3 inhibitors via virtual screening and in vitro bioassay
Jie Xia, Huabin Hu, Wenjie Xue, Xiang Simon Wang & Song Wu
Pages: 525-535
Published online: 21 Feb 2018
AbstractforThe discovery of novel HDAC3 inhibitors via virtual screening and in vitro bioassay | Full Text | References | PDF (2.7 MB) | Supplemental
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Article
Synthesis and biological evaluation of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential antiplatelet agents
Monika Marcinkowska, Magdalena Kotańska, Agnieszka Zagórska, Joanna Śniecikowska, Monika Kubacka, Agata Siwek, Adam Bucki, Maciej Pawłowski, Marek Bednarski, Jacek Sapa, Małgorzata Starek, Monika Dąbrowska & Marcin Kołaczkowski
Pages: 536-545
Published online: 27 Feb 2018
AbstractforSynthesis and biological evaluation of N-arylpiperazine derivatives of 4,4-dimethylisoquinoline-1,3(2H,4H)-dione as potential antiplatelet agents | Full Text | References | PDF (1.3 MB)
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Article
Anticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold
Heba S. A. Elzahabi, Eman S. Nossier, Nagy M. Khalifa, Rania A. Alasfoury & May A. El-Manawaty
Pages: 546-557
Published online: 27 Feb 2018
AbstractforAnticancer evaluation and molecular modeling of multi-targeted kinase inhibitors based pyrido[2,3-d]pyrimidine scaffold | Full Text | References | PDF (2.2 MB)
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Corrigendum

Correction
Correction to: New cyclopentaquinoline hybrids with multifunctional capacities for the treatment of Alzheimer’s disease
Pages: 558-559
Published online: 13 Mar 2018
CitationforCorrection to: New cyclopentaquinoline hybrids with multifunctional capacities for the treatment of Alzheimer’s disease | Full Text | References | PDF (365.4 KB)
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Article
Antinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2
Justyna Piekielna-Ciesielska, Adriano Mollica, Stefano Pieretti, Jakub Fichna, Agata Szymaszkiewicz, Marta Zielińska, Radzisław Kordek & Anna Janecka
Pages: 560-566
Published online: 07 Mar 2018
AbstractforAntinociceptive potency of a fluorinated cyclopeptide Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 | Full Text | References | PDF (1 MB)
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Article
Discovery of a new mitochondria permeability transition pore (mPTP) inhibitor based on gallic acid
José Teixeira, Catarina Oliveira, Fernando Cagide, Ricardo Amorim, Jorge Garrido, Fernanda Borges & Paulo J. Oliveira
Pages: 567-576
Published online: 07 Mar 2018
AbstractforDiscovery of a new mitochondria permeability transition pore (mPTP) inhibitor based on gallic acid | Full Text | References | PDF (2 MB)
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Article
Isothiocyanates: cholinesterase inhibiting, antioxidant, and anti-inflammatory activity
Franko Burčul, Ivana Generalić Mekinić, Mila Radan, Patrick Rollin & Ivica Blažević
Pages: 577-582
Published online: 07 Mar 2018
AbstractforIsothiocyanates: cholinesterase inhibiting, antioxidant, and anti-inflammatory activity | Full Text | References | PDF (1.2 MB)
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Review Article

Review
Profiling donepezil template into multipotent hybrids with antioxidant properties
Eva Mezeiova, Katarina Spilovska, Eugenie Nepovimova, Lukas Gorecki, Ondrej Soukup, Rafael Dolezal, David Malinak, Jana Janockova, Daniel Jun, Kamil Kuca & Jan Korabecny
Pages: 583-606
Published online: 13 Mar 2018
AbstractforProfiling donepezil template into multipotent hybrids with antioxidant properties | Full Text | References | PDF (3.9 MB)
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Article
The hop-derived compounds xanthohumol, isoxanthohumol and 8-prenylnaringenin are tight-binding inhibitors of human aldo-keto reductases 1B1 and 1B10
Jan Moritz Seliger, Livia Misuri, Edmund Maser & Jan Hintzpeter
Pages: 607-614
Published online: 13 Mar 2018
AbstractforThe hop-derived compounds xanthohumol, isoxanthohumol and 8-prenylnaringenin are tight-binding inhibitors of human aldo-keto reductases 1B1 and 1B10 | Full Text | References | PDF (1 MB)
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Article
Iodine-mediated one-pot intramolecular decarboxylation domino reaction for accessing functionalised 2-(1,3,4-oxadiazol-2-yl)anilines with carbonic anhydrase inhibitory action
Srinivas Angapelly, P. V. Sri Ramya, Rohini Sodhi, Andrea Angeli, Krishnan Rangan, Narayana Nagesh, Claudiu T. Supuran & Mohammed Arifuddin
Pages: 615-628
Published online: 14 Mar 2018
AbstractforIodine-mediated one-pot intramolecular decarboxylation domino reaction for accessing functionalised 2-(1,3,4-oxadiazol-2-yl)anilines with carbonic anhydrase inhibitory action | Full Text | References | PDF (1.8 MB)
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Article
Inhibition studies on a panel of human carbonic anhydrases with N1-substituted secondary sulfonamides incorporating thiazolinone or imidazolone-indole tails
Fadi M. Awadallah, Silvia Bua, Walaa R. Mahmoud, Hossam H. Nada, Alessio Nocentini & Claudiu T. Supuran
Pages: 629-638
Published online: 14 Mar 2018
AbstractforInhibition studies on a panel of human carbonic anhydrases with N1-substituted secondary sulfonamides incorporating thiazolinone or imidazolone-indole tails | Full Text | References | PDF (1.2 MB)
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Article
Inhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds
Sylwia Bloch, Bożena Nejman-Faleńczyk, Karolina Pierzynowska, Ewa Piotrowska, Alicja Węgrzyn, Christelle Marminon, Zouhair Bouaziz, Pascal Nebois, Joachim Jose, Marc Le Borgne, Luciano Saso & Grzegorz Węgrzyn
Pages: 639-650
Published online: 14 Mar 2018
AbstractforInhibition of Shiga toxin-converting bacteriophage development by novel antioxidant compounds | Full Text | References | PDF (2.9 MB) | Supplemental
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Short Communication

Rapid Communication
Introduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors
Minhang Xin, Weiming Duan, Yifan Feng, Yuan-Yuan Hei, Hao Zhang, Ying Shen, Hong-Yi Zhao, Shuai Mao & San-Qi Zhang
Pages: 651-656
Published online: 14 Mar 2018
AbstractforIntroduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors | Full Text | References | PDF (2 MB)
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Research Paper

Article
Molecular cloning and anti-invasive activity of cathepsin L propeptide-like protein from Calotropis procera R. Br. against cancer cells
Chang Woo Kwon, Hee Yang, SuBin Yeo, Kyung-Min Park, Ae Jin Jeong, Ki Won Lee, Sang-Kyu Ye & Pahn-Shick Chang
Pages: 657-664
Published online: 21 Mar 2018
AbstractforMolecular cloning and anti-invasive activity of cathepsin L propeptide-like protein from Calotropis procera R. Br. against cancer cells | Full Text | References | PDF (1.2 MB) | Supplemental
  • 1503 Views
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Short Communication

Rapid Communication
1-(Benzo[d]thiazol-2-yl)-3-phenylureas as dual inhibitors of casein kinase 1 and ABAD enzymes for treatment of neurodegenerative disorders
Ondrej Benek, Lukas Hroch, Laura Aitken, Frank Gunn-Moore, Lucie Vinklarova, Kamil Kuca, Daniel I. Perez, Concepcion Perez, Ana Martinez, Zdenek Fisar & Kamil Musilek
Pages: 665-670
Published online: 14 Mar 2018
Abstractfor1-(Benzo[d]thiazol-2-yl)-3-phenylureas as dual inhibitors of casein kinase 1 and ABAD enzymes for treatment of neurodegenerative disorders | Full Text | References | PDF (1.8 MB)
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Research Paper

Article
Resolution of co-eluting isomers of anti-inflammatory drugs conjugated to carbonic anhydrase inhibitors from plasma in liquid chromatography by energy-resolved tandem mass spectrometry
Marta Menicatti, Marco Pallecchi, Silvia Bua, Daniela Vullo, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Fabrizio Carta, Claudiu T. Supuran & Gianluca Bartolucci
Pages: 671-679
Published online: 14 Mar 2018
AbstractforResolution of co-eluting isomers of anti-inflammatory drugs conjugated to carbonic anhydrase inhibitors from plasma in liquid chromatography by energy-resolved tandem mass spectrometry | Full Text | References | PDF (1.6 MB) | Supplemental
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Short Communication

Rapid Communication
The first activation study of a δ-carbonic anhydrase: TweCAδ from the diatom Thalassiosira weissflogii is effectively activated by amines and amino acids
Andrea Angeli, Fatmah A. S. Alasmary, Sonia Del Prete, Sameh M. Osman, Zeid AlOthman, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 680-685
Published online: 14 Mar 2018
AbstractforThe first activation study of a δ-carbonic anhydrase: TweCAδ from the diatom Thalassiosira weissflogii is effectively activated by amines and amino acids | Full Text | References | PDF (720.8 KB)
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Research Paper

Article
Novel [(3-indolylmethylene)hydrazono]indolin-2-ones as apoptotic anti-proliferative agents: design, synthesis and in vitro biological evaluation
Wagdy M. Eldehna, Mahmoud F. Abo-Ashour, Hany S. Ibrahim, Ghada H. Al-Ansary, Hazem A. Ghabbour, Mahmoud M. Elaasser, Hanaa Y. A. Ahmed & Nesreen A. Safwat
Pages: 686-700
Published online: 21 Mar 2018
AbstractforNovel [(3-indolylmethylene)hydrazono]indolin-2-ones as apoptotic anti-proliferative agents: design, synthesis and in vitro biological evaluation | Full Text | References | PDF (1.9 MB) | Supplemental
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Article
Identification of cisplatin-binding sites on the large cytoplasmic loop of the Na+/K+-ATPase
Jaroslava Šeflová, Petra Čechová, Tereza Štenclová, Marek Šebela & Martin Kubala
Pages: 701-706
Published online: 26 Mar 2018
AbstractforIdentification of cisplatin-binding sites on the large cytoplasmic loop of the Na+/K+-ATPase | Full Text | References | PDF (1.9 MB) | Supplemental
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Short Communication

Rapid Communication
Mono- and di-thiocarbamate inhibition studies of the δ-carbonic anhydrase TweCAδ from the marine diatom Thalassiosira weissflogii
Silvia Bua, Murat Bozdag, Sonia Del Prete, Fabrizio Carta, William A. Donald, Clemente Capasso & Claudiu T. Supuran
Pages: 707-713
Published online: 26 Mar 2018
AbstractforMono- and di-thiocarbamate inhibition studies of the δ-carbonic anhydrase TweCAδ from the marine diatom Thalassiosira weissflogii | Full Text | References | PDF (1.1 MB)
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Review Article

Review
Zinc binding groups for histone deacetylase inhibitors
Lei Zhang, Jian Zhang, Qixiao Jiang, Li Zhang & Weiguo Song
Pages: 714-721
Published online: 04 Apr 2018
AbstractforZinc binding groups for histone deacetylase inhibitors | Full Text | References | PDF (1.4 MB)
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Research Paper

Article
Designing a new biosensor “DNA ELISA” to detect Escherichia coli using genomic DNA and comparison of this method to PCR-ELISA
Elaheh Hashemi & Mehdi Forouzandeh
Pages: 722-725
Published online: 04 Apr 2018
AbstractforDesigning a new biosensor “DNA ELISA” to detect Escherichia coli using genomic DNA and comparison of this method to PCR-ELISA | Full Text | References | PDF (649.8 KB)
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Corrigendum

Correction
Correction to: Inhibitors of alanine racemase enzyme: a review
Page: 726
Published online: 10 Apr 2018
CitationforCorrection to: Inhibitors of alanine racemase enzyme: a review | Full Text | PDF (134 KB)
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Research Paper

Article
Synthesis and biological evaluation of alpha-bromoacryloylamido indolyl pyridinyl propenones as potent apoptotic inducers in human leukaemia cells
Romeo Romagnoli, Filippo Prencipe, Luisa Carlota Lopez-Cara, Paola Oliva, Stefania Baraldi, Pier Giovanni Baraldi, Francisco Estévez-Sarmiento, José Quintana & Francisco Estévez
Pages: 727-742
Published online: 05 Apr 2018
AbstractforSynthesis and biological evaluation of alpha-bromoacryloylamido indolyl pyridinyl propenones as potent apoptotic inducers in human leukaemia cells | Full Text | References | PDF (2 MB) | Supplemental
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Article
Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives
Sanna Niinivehmas, Pekka A. Postila, Sanna Rauhamäki, Elangovan Manivannan, Sami Kortet, Mira Ahinko, Pasi Huuskonen, Niina Nyberg, Pasi Koskimies, Sakari Lätti, Elina Multamäki, Risto O. Juvonen, Hannu Raunio, Markku Pasanen, Juhani Huuskonen & Olli T. Pentikäinen
Pages: 743-754
Published online: 05 Apr 2018
AbstractforBlocking oestradiol synthesis pathways with potent and selective coumarin derivatives | Full Text | References | PDF (3.2 MB)
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Article
Molecular modelling insights into a physiologically favourable approach to eicosanoid biosynthesis inhibition through novel thieno[2,3-b]pyridine derivatives
Mosaad S. Mohamed, Yara E. Mansour, Hatem K. Amin & Moustafa E. El-Araby
Pages: 755-767
Published online: 13 Apr 2018
AbstractforMolecular modelling insights into a physiologically favourable approach to eicosanoid biosynthesis inhibition through novel thieno[2,3-b]pyridine derivatives | Full Text | References | PDF (2.6 MB) | Supplemental
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Article
Novel hits for acetylcholinesterase inhibition derived by docking-based screening on ZINC database
Irini Doytchinova, Mariyana Atanasova, Iva Valkova, Georgi Stavrakov, Irena Philipova, Zvetanka Zhivkova, Dimitrina Zheleva-Dimitrova, Spiro Konstantinov & Ivan Dimitrov
Pages: 768-776
Published online: 13 Apr 2018
AbstractforNovel hits for acetylcholinesterase inhibition derived by docking-based screening on ZINC database | Full Text | References | PDF (2.1 MB) | Supplemental
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Review Article

Review
Small molecule KDM4s inhibitors as anti-cancer agents
Hongzhi Lin, Qihang Li, Qi Li, Jie Zhu, Kai Gu, Xueyang Jiang, Qianqian Hu, Feng Feng, Wei Qu, Yao Chen & Haopeng Sun
Pages: 777-793
Published online: 13 Apr 2018
AbstractforSmall molecule KDM4s inhibitors as anti-cancer agents | Full Text | References | PDF (4.2 MB)
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Research Paper

Article
Kinetic and structural studies on the interactions of Torpedo californica acetylcholinesterase with two donepezil-like rigid analogues
Rosanna Caliandro, Alessandro Pesaresi, Luca Cariati, Antonio Procopio, Manuela Oliverio & Doriano Lamba
Pages: 794-803
Published online: 13 Apr 2018
AbstractforKinetic and structural studies on the interactions of Torpedo californica acetylcholinesterase with two donepezil-like rigid analogues | Full Text | References | PDF (2.7 MB)
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Short Communication

Rapid Communication
Fluoroenesulphonamides: N-sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition
Benoit Métayer, Andrea Angeli, Agnès Mingot, Kévin Jouvin, Gwilherm Evano, Claudiu T. Supuran & Sébastien Thibaudeau
Pages: 804-808
Published online: 30 Apr 2018
AbstractforFluoroenesulphonamides: N-sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition | Full Text | References | PDF (1 MB)
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Article
Synthesis and evaluation of novel spiro derivatives for pyrrolopyrimidines as anti-hyperglycemia promising compounds
Samar Said Fatahala, Shahenda Mahgub, Heba Taha & Rania Helmy Abd-El Hameed
Pages: 809-817
Published online: 30 Apr 2018
First Page PreviewforSynthesis and evaluation of novel spiro derivatives for pyrrolopyrimidines as anti-hyperglycemia promising compounds | Full Text | References | PDF (1.1 MB) | Supplemental
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Article
Synthesis, antimicrobial, anti-biofilm evaluation, and molecular modelling study of new chalcone linked amines derivatives
Shahenda M. El-Messery, El-Sayed E. Habib, Sarah T. A. Al-Rashood & Ghada S. Hassan
Pages: 818-832
Published online: 03 May 2018
AbstractforSynthesis, antimicrobial, anti-biofilm evaluation, and molecular modelling study of new chalcone linked amines derivatives | Full Text | References | PDF (3.6 MB) | Supplemental
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Article
Identification of a novel small-molecule Keap1–Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy
Cheng-Shi Jiang, Chun-Lin Zhuang, Kongkai Zhu, Juan Zhang, Luis Alexandre Muehlmann, João Paulo Figueiró Longo, Ricardo Bentes Azevedo, Wen Zhang, Ning Meng & Hua Zhang
Pages: 833-841
Published online: 25 Apr 2018
AbstractforIdentification of a novel small-molecule Keap1–Nrf2 PPI inhibitor with cytoprotective effects on LPS-induced cardiomyopathy | Full Text | References | PDF (1.8 MB) | Supplemental
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Article
The RFK catalytic cycle of the pathogen Streptococcus pneumoniae shows species-specific features in prokaryotic FMN synthesis
María Sebastián, Adrián Velázquez-Campoy & Milagros Medina
Pages: 842-849
Published online: 25 Apr 2018
AbstractforThe RFK catalytic cycle of the pathogen Streptococcus pneumoniae shows species-specific features in prokaryotic FMN synthesis | Full Text | References | PDF (2.2 MB) | Supplemental
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Article
Antileishmanial activity of sulphonamide nanoemulsions targeting the β-carbonic anhydrase from Leishmania species
Verônica da Silva Cardoso, Alane Beatriz Vermelho, Eduardo Ricci Junior, Igor Almeida Rodrigues, Ana Maria Mazotto & Claudiu T. Supuran
Pages: 850-857
Published online: 30 Apr 2018
AbstractforAntileishmanial activity of sulphonamide nanoemulsions targeting the β-carbonic anhydrase from Leishmania species | Full Text | References | PDF (1.2 MB)
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Article
Structural re-positioning, in silico molecular modelling, oxidative degradation, and biological screening of linagliptin as adenosine 3 receptor (ADORA3) modulators targeting hepatocellular carcinoma
Bassam M. Ayoub, Yasmeen M. Attia & Mahmoud S. Ahmed
Pages: 858-866
Published online: 16 May 2018
AbstractforStructural re-positioning, in silico molecular modelling, oxidative degradation, and biological screening of linagliptin as adenosine 3 receptor (ADORA3) modulators targeting hepatocellular carcinoma | Full Text | References | PDF (2.5 MB) | Supplemental
  • 1731 Views
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Article
Synthesis and biological evaluation of certain hydrazonoindolin-2-one derivatives as new potent anti-proliferative agents
Wagdy M. Eldehna, Reem I. Al-Wabli, Maha S. Almutairi, Adam B. Keeton, Gary A. Piazza, Hatem A. Abdel-Aziz & Mohamed I. Attia
Pages: 867-878
Published online: 30 Apr 2018
AbstractforSynthesis and biological evaluation of certain hydrazonoindolin-2-one derivatives as new potent anti-proliferative agents | Full Text | References | PDF (1.9 MB)
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Article
Antibacterial activity of 3-methylbenzo[d]thiazol-methylquinolinium derivatives and study of their action mechanism
Ning Sun, Ruo-Lan Du, Yuan-Yuan Zheng, Qi Guo, Sen-Yuan Cai, Zhi-Hua Liu, Zhi-Yuan Fang, Wen-Chang Yuan, Ting Liu, Xiao-Mei Li, Yu-Jing Lu & Kwok-Yin Wong
Pages: 879-889
Published online: 03 May 2018
AbstractforAntibacterial activity of 3-methylbenzo[d]thiazol-methylquinolinium derivatives and study of their action mechanism | Full Text | References | PDF (2.3 MB) | Supplemental
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Review
Advances in the discovery of cathepsin K inhibitors on bone resorption
Jun Lu, Maolin Wang, Ziyue Wang, Zhongqi Fu, Aiping Lu & Ge Zhang
Pages: 890-904
Published online: 03 May 2018
AbstractforAdvances in the discovery of cathepsin K inhibitors on bone resorption | Full Text | References | PDF (2.9 MB)
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Article
Design, synthesis and biological evaluation of 4-bromo-N-(3,5-dimethoxyphenyl)benzamide derivatives as novel FGFR1 inhibitors for treatment of non-small cell lung cancer
Zixin Xie, Donghua Cheng, Lu Luo, Guoliang Shen, Suwei Pan, Yaqian Pan, Bo Chen, Xuebao Wang, Zhiguo Liu, Yuan Zhang & Faqing Ye
Pages: 905-919
Published online: 07 May 2018
AbstractforDesign, synthesis and biological evaluation of 4-bromo-N-(3,5-dimethoxyphenyl)benzamide derivatives as novel FGFR1 inhibitors for treatment of non-small cell lung cancer | Full Text | References | PDF (3.4 MB) | Supplemental
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Article
Pentabromopseudilin: a myosin V inhibitor suppresses TGF-β activity by recruiting the type II TGF-β receptor to lysosomal degradation
Wang Shih-Wei, Chung Chih-Ling, Yu-Chen Kao, René Martin, Hans-Joachim Knölker, Meng-Shin Shiao & Chun-Lin Chen
Pages: 920-935
Published online: 16 May 2018
AbstractforPentabromopseudilin: a myosin V inhibitor suppresses TGF-β activity by recruiting the type II TGF-β receptor to lysosomal degradation | Full Text | References | PDF (5.5 MB) | Supplemental
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Article
UHPLC-ESI-ORBITRAP-MS analysis of the native Mapuche medicinal plant palo negro (Leptocarpha rivularis DC. – Asteraceae) and evaluation of its antioxidant and cholinesterase inhibitory properties
Andrea Jiménez-González, Cristina Quispe, Jorge Bórquez, Beatriz Sepúlveda, Felipe Riveros, Carlos Areche, Edgar Nagles, Olimpo García-Beltrán & Mario J. Simirgiotis
Pages: 936-944
Published online: 07 May 2018
AbstractforUHPLC-ESI-ORBITRAP-MS analysis of the native Mapuche medicinal plant palo negro (Leptocarpha rivularis DC. – Asteraceae) and evaluation of its antioxidant and cholinesterase inhibitory properties | Full Text | References | PDF (1.4 MB) | Supplemental
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Article
Activation of β- and γ-carbonic anhydrases from pathogenic bacteria with tripeptides
Azzurra Stefanucci, Andrea Angeli, Marilisa Pia Dimmito, Grazia Luisi, Sonia Del Prete, Clemente Capasso, William A. Donald, Adriano Mollica & Claudiu T. Supuran
Pages: 945-950
Published online: 11 May 2018
AbstractforActivation of β- and γ-carbonic anhydrases from pathogenic bacteria with tripeptides | Full Text | References | PDF (663.4 KB)
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Article
Determination and diagnostic value of CA9 mRNA in peripheral blood of patients with oral leukoplakia
Manuel Torres López, Mario Pérez Sayáns, Cintia Chamorro Petronacci, Francisco Barros Angueira, Pilar Gándara Vila, Alejandro Lorenzo Pouso & Abel García García
Pages: 951-955
Published online: 10 May 2018
AbstractforDetermination and diagnostic value of CA9 mRNA in peripheral blood of patients with oral leukoplakia | Full Text | References | PDF (915.5 KB) | Supplemental
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Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors
Giulio Poli, Margherita Lapillo, Carlotta Granchi, Jessica Caciolla, Nayla Mouawad, Isabella Caligiuri, Flavio Rizzolio, Thierry Langer, Filippo Minutolo & Tiziano Tuccinardi
Pages: 956-961
Published online: 11 May 2018
AbstractforBinding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors | Full Text | References | PDF (1.4 MB) | Supplemental
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Article
Evaluation of sulphonamide derivatives acting as inhibitors of human carbonic anhydrase isoforms I, II and Mycobacterium tuberculosisβ-class enzyme Rv3273
Tanvi V. Wani, Silvia Bua, Pravin S. Khude, Abdul H. Chowdhary, Claudiu T. Supuran & Mrunmayee P. Toraskar
Pages: 962-971
Published online: 18 May 2018
AbstractforEvaluation of sulphonamide derivatives acting as inhibitors of human carbonic anhydrase isoforms I, II and Mycobacterium tuberculosisβ-class enzyme Rv3273 | Full Text | References | PDF (947.7 KB)
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Newer human inosine 5′-monophosphate dehydrogenase 2 (hIMPDH2) inhibitors as potential anticancer agents
Chetan P. Shah & Prashant S. Kharkar
Pages: 972-977
Published online: 24 May 2018
AbstractforNewer human inosine 5′-monophosphate dehydrogenase 2 (hIMPDH2) inhibitors as potential anticancer agents | Full Text | References | PDF (1 MB) | Supplemental
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Article
Synthesis and in vivo anti-ulcer evaluation of some novel piperidine linked dihydropyrimidinone derivatives
Mashooq Ahmad Bhat, Mohamed A. Al-Omar & Ahmed M. Naglah
Pages: 978-988
Published online: 24 May 2018
AbstractforSynthesis and in vivo anti-ulcer evaluation of some novel piperidine linked dihydropyrimidinone derivatives | Full Text | References | PDF (2.2 MB)
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Article
Synthesis, antitumour activities and molecular docking of thiocarboxylic acid ester-based NSAID scaffolds: COX-2 inhibition and mechanistic studies
Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Laila A. Abou-Zeid, Walaa M. El-Husseiny, Ahmad M. El_Morsy, Manal A. El-Gendy & Magda A.-A. El-Sayed
Pages: 989-998
Published online: 28 May 2018
AbstractforSynthesis, antitumour activities and molecular docking of thiocarboxylic acid ester-based NSAID scaffolds: COX-2 inhibition and mechanistic studies | Full Text | References | PDF (2.3 MB) | Supplemental
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Article
Dioxygen, an unexpected carbonic anhydrase ligand
Marta Ferraroni, Roberto Gaspari, Andrea Scozzafava, Andrea Cavalli & Claudiu T. Supuran
Pages: 999-1005
Published online: 28 May 2018
AbstractforDioxygen, an unexpected carbonic anhydrase ligand | Full Text | References | PDF (1.6 MB)
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Article
A novel series of pyrazole-platinum(II) complexes as potential anti-cancer agents that induce cell cycle arrest and apoptosis in breast cancer cells
Robert Czarnomysy, Arkadiusz Surażyński, Anna Muszynska, Agnieszka Gornowicz, Anna Bielawska & Krzysztof Bielawski
Pages: 1006-1023
Published online: 04 Jun 2018
AbstractforA novel series of pyrazole-platinum(II) complexes as potential anti-cancer agents that induce cell cycle arrest and apoptosis in breast cancer cells | Full Text | References | PDF (3.9 MB) | Supplemental
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Article
CAIX furthers tumour progression in the hypoxic tumour microenvironment of esophageal carcinoma and is a possible therapeutic target
Astrid Drenckhan, Morton Freytag, Claudiu T. Supuran, Guido Sauter, Jakob R. Izbicki & Stephanie J. Gros
Pages: 1024-1033
Published online: 04 Jun 2018
AbstractforCAIX furthers tumour progression in the hypoxic tumour microenvironment of esophageal carcinoma and is a possible therapeutic target | Full Text | References | PDF (1.4 MB)
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Article
Identification of new allosteric sites and modulators of AChE through computational and experimental tools
Carlos Roca, Carlos Requena, Víctor Sebastián-Pérez, Sony Malhotra, Chris Radoux, Concepción Pérez, Ana Martinez, Juan Antonio Páez, Tom L. Blundell & Nuria E. Campillo
Pages: 1034-1047
Published online: 06 Jun 2018
AbstractforIdentification of new allosteric sites and modulators of AChE through computational and experimental tools | Full Text | References | PDF (5.5 MB) | Supplemental
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Article
Kushenol A and 8-prenylkaempferol, tyrosinase inhibitors, derived from Sophora flavescens
Jang Hoon Kim, In Sook Cho, Yang Kang So, Hyeong-Hwan Kim & Young Ho Kim
Pages: 1048-1054
Published online: 06 Jun 2018
AbstractforKushenol A and 8-prenylkaempferol, tyrosinase inhibitors, derived from Sophora flavescens | Full Text | References | PDF (1.8 MB) | Supplemental
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Short Communication

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Oregonin from Alnus incana bark affects DNA methyltransferases expression and mitochondrial DNA copies in mouse embryonic fibroblasts
Jelena Krasilnikova, Liga Lauberte, Elena Stoyanova, Desislava Abadjieva, Mihail Chervenkov, Mattia Mori, Elisa De Paolis, Vanya Mladenova, Galina Telysheva, Bruno Botta & Elena Kistanova
Pages: 1055-1063
Published online: 07 Jun 2018
AbstractforOregonin from Alnus incana bark affects DNA methyltransferases expression and mitochondrial DNA copies in mouse embryonic fibroblasts | Full Text | References | PDF (1.8 MB)
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Article
Nitroimidazole-based inhibitors DTP338 and DTP348 are safe for zebrafish embryos and efficiently inhibit the activity of human CA IX in Xenopus oocytes
Ashok Aspatwar, Holger M. Becker, Nanda Kumar Parvathaneni, Milka Hammaren, Aleksandra Svorjova, Harlan Barker, Claudiu T. Supuran, Ludwig Dubois, Philippe Lambin, Mataleena Parikka, Seppo Parkkila & Jean-Yves Winum
Pages: 1064-1073
Published online: 17 Jun 2018
AbstractforNitroimidazole-based inhibitors DTP338 and DTP348 are safe for zebrafish embryos and efficiently inhibit the activity of human CA IX in Xenopus oocytes | Full Text | References | PDF (3 MB)
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Article
Introducing novel potent anticancer agents of 1H-benzo[f]chromene scaffolds, targeting c-Src kinase enzyme with MDA-MB-231 cell line anti-invasion effect
Hany E. A. Ahmed, Mohammed A. A. El-Nassag, Ahmed H. Hassan, Rawda M. Okasha, Saleh Ihmaid, Ahmed M. Fouda, Tarek H. Afifi, Ateyatallah Aljuhani & Ahmed M. El-Agrody
Pages: 1074-1088
Published online: 20 Jun 2018
AbstractforIntroducing novel potent anticancer agents of 1H-benzo[f]chromene scaffolds, targeting c-Src kinase enzyme with MDA-MB-231 cell line anti-invasion effect | Full Text | References | PDF (2.2 MB) | Supplemental
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A highly potent and selective inhibitor Roxyl-WL targeting IDO1 promotes immune response against melanoma
Guangwei Xu, Tianqi Wang, Yongtao Li, Zhi Huang, Xin Wang, Jianyu Zheng, Shengyong Yang, Yan Fan & Rong Xiang
Pages: 1089-1094
Published online: 22 Jun 2018
AbstractforA highly potent and selective inhibitor Roxyl-WL targeting IDO1 promotes immune response against melanoma | Full Text | References | PDF (1.5 MB) | Supplemental
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Article
Novel coumarin-6-sulfonamides as apoptotic anti-proliferative agents: synthesis, in vitro biological evaluation, and QSAR studies
Ahmed Sabt, Omaima M. Abdelhafez, Radwan S. El-Haggar, Hassan M. F. Madkour, Wagdy M. Eldehna, Ezz El-Din A. M. El-Khrisy, Mohamed A. Abdel-Rahman & Laila. A. Rashed
Pages: 1095-1107
Published online: 26 Jun 2018
AbstractforNovel coumarin-6-sulfonamides as apoptotic anti-proliferative agents: synthesis, in vitro biological evaluation, and QSAR studies | Full Text | References | PDF (1.7 MB) | Supplemental
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Article
Synthesis, biological evaluation, and molecular modelling studies of potent human neutrophil elastase (HNE) inhibitors
Maria Paola Giovannoni, Igor A. Schepetkin, Mark T. Quinn, Niccolò Cantini, Letizia Crocetti, Gabriella Guerrini, Antonella Iacovone, Paola Paoli, Patrizia Rossi, Gianluca Bartolucci, Marta Menicatti & Claudia Vergelli
Pages: 1108-1124
Published online: 04 Jul 2018
AbstractforSynthesis, biological evaluation, and molecular modelling studies of potent human neutrophil elastase (HNE) inhibitors | Full Text | References | PDF (4 MB) | Supplemental
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Article
Synthesis of novel benzenesulfamide derivatives with inhibitory activity against human cytosolic carbonic anhydrase I and II and Vibrio cholerae α- and β-class enzymes
Silvia Bua, Emanuela Berrino, Sonia Del Prete, Vallabhaneni S. Murthy, Vijayaparthasarathi Vijayakumar, Yasinalli Tamboli, Clemente Capasso, Elisabetta Cerbai, Alessandro Mugelli, Fabrizio Carta & Claudiu T. Supuran
Pages: 1125-1136
Published online: 10 Jul 2018
AbstractforSynthesis of novel benzenesulfamide derivatives with inhibitory activity against human cytosolic carbonic anhydrase I and II and Vibrio cholerae α- and β-class enzymes | Full Text | References | PDF (1.5 MB)
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Article
Selective inhibition of carbonic anhydrase-IX by sulphonamide derivatives induces pH and reactive oxygen species-mediated apoptosis in cervical cancer HeLa cells
Ismail Koyuncu, Ataman Gonel, Abdurrahim Kocyigit, Ebru Temiz, Mustafa Durgun & Claudiu T. Supuran
Pages: 1137-1149
Published online: 12 Jul 2018
AbstractforSelective inhibition of carbonic anhydrase-IX by sulphonamide derivatives induces pH and reactive oxygen species-mediated apoptosis in cervical cancer HeLa cells | Full Text | References | PDF (3.8 MB)
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Article
Synthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes
Mehdi Bouchouit, Sofiane Bouacida, Bachir Zouchoune, Hocine Merazig, Silvia Bua, Zouhair Bouaziz, Marc Le Borgne, Claudiu T. Supuran & Abdelmalek Bouraiou
Pages: 1150-1159
Published online: 13 Jul 2018
AbstractforSynthesis, X-ray structure, in silico calculation, and carbonic anhydrase inhibitory properties of benzylimidazole metal complexes | Full Text | References | PDF (2.3 MB) | Supplemental
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Article
Pyrrolo[3,2-c]pyridine derivatives with potential inhibitory effect against FMS kinase: in vitro biological studies
Mohammed I. El-Gamal & Chang-Hyun Oh
Pages: 1160-1166
Published online: 02 Aug 2018
AbstractforPyrrolo[3,2-c]pyridine derivatives with potential inhibitory effect against FMS kinase: in vitro biological studies | Full Text | References | PDF (2 MB) | Supplemental
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The effects of phenolic glycosides from Betula platyphylla var. japonica on adipocyte differentiation and mature adipocyte metabolism
Joo Young Huh, Seulah Lee, Eun-Bi Ma, Hee Jeong Eom, Jiwon Baek, Yoon-Joo Ko & Ki Hyun Kim
Pages: 1167-1173
Published online: 21 Aug 2018
AbstractforThe effects of phenolic glycosides from Betula platyphylla var. japonica on adipocyte differentiation and mature adipocyte metabolism | Full Text | References | PDF (1.7 MB) | Supplemental
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Article
The insight of in vitro and in silico studies on cholinesterase inhibitors from the roots of Cimicifuga dahurica (Turcz.) Maxim.
Jang Hoon Kim, Nguyen Phuong Thao, Yoo Kyong Han, Young Suk Lee, Bui Thi Thuy Luyen, Ha Van Oanh, Young Ho Kim & Seo Young Yang
Pages: 1174-1180
Published online: 05 Oct 2018
AbstractforThe insight of in vitro and in silico studies on cholinesterase inhibitors from the roots of Cimicifuga dahurica (Turcz.) Maxim. | Full Text | References | PDF (2.2 MB) | Supplemental
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Article
Synthesis and pharmacological evaluation of novel isoquinoline N-sulphonylhydrazones designed as ROCK inhibitors
Ramon Guerra de Oliveira, Fabiana Sélos Guerra, Cláudia dos Santos Mermelstein, Patrícia Dias Fernandes, Isadora Tairinne de Sena Bastos, Fanny Nascimento Costa, Regina Cely Rodrigues Barroso, Fabio Furlan Ferreira & Carlos Alberto Manssour Fraga
Pages: 1181-1193
Published online: 25 Jul 2018
AbstractforSynthesis and pharmacological evaluation of novel isoquinoline N-sulphonylhydrazones designed as ROCK inhibitors | Full Text | References | PDF (3.3 MB) | Supplemental
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Article
Inhibition of α-, β-, γ-, and δ-carbonic anhydrases from bacteria and diatoms with N′-aryl-N-hydroxy-ureas
Emanuela Berrino, Murat Bozdag, Sonia Del Prete, Fatmah A. S. Alasmary, Linah S. Alqahtani, Zeid AlOthman, Clemente Capasso & Claudiu T. Supuran
Pages: 1194-1198
Published online: 25 Jul 2018
AbstractforInhibition of α-, β-, γ-, and δ-carbonic anhydrases from bacteria and diatoms with N′-aryl-N-hydroxy-ureas | Full Text | References | PDF (739.8 KB)
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Discovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin
Jie Quan Wang, Meng Di Yang, Xing Chen, Yang Wang, Liu Zeng Chen, Xiu Cheng & Xin Hua Liu
Pages: 1199-1211
Published online: 22 Aug 2018
AbstractforDiscovery of new chromen-4-one derivatives as telomerase inhibitors through regulating expression of dyskerin | Full Text | References | PDF (3.1 MB) | Supplemental
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Article
Donepezil structure-based hybrids as potential multifunctional anti-Alzheimer’s drug candidates
Luca Piemontese, Daniel Tomás, Asha Hiremathad, Vito Capriati, Emanuel Candeias, Sandra M. Cardoso, Sílvia Chaves & M. Amélia Santos
Pages: 1212-1224
Published online: 30 Aug 2018
AbstractforDonepezil structure-based hybrids as potential multifunctional anti-Alzheimer’s drug candidates | Full Text | References | PDF (2.8 MB) | Supplemental
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Article
Design, synthesis, in vitro antiproliferative activity and apoptosis-inducing studies of 1-(3′,4′,5′-trimethoxyphenyl)-3-(2′-alkoxycarbonylindolyl)-2-propen-1-one derivatives obtained by a molecular hybridisation approach
Delia Preti, Romeo Romagnoli, Riccardo Rondanin, Barbara Cacciari, Ernest Hamel, Jan Balzarini, Sandra Liekens, Dominique Schols, Francisco Estévez-Sarmiento, José Quintana & Francisco Estévez
Pages: 1225-1238
Published online: 24 Aug 2018
AbstractforDesign, synthesis, in vitro antiproliferative activity and apoptosis-inducing studies of 1-(3′,4′,5′-trimethoxyphenyl)-3-(2′-alkoxycarbonylindolyl)-2-propen-1-one derivatives obtained by a molecular hybridisation approach | Full Text | References | PDF (2.1 MB) | Supplemental
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Article
Discovery of (phenylureido)piperidinyl benzamides as prospective inhibitors of bacterial autolysin E from Staphylococcus aureus
Jure Borišek, Sara Pintar, Mitja Ogrizek, Simona Golič Grdadolnik, Vesna Hodnik, Dušan Turk, Andrej Perdih & Marjana Novič
Pages: 1239-1247
Published online: 24 Aug 2018
AbstractforDiscovery of (phenylureido)piperidinyl benzamides as prospective inhibitors of bacterial autolysin E from Staphylococcus aureus | Full Text | References | PDF (2.7 MB) | Supplemental
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Article
Novel imidazopyridine suppresses STAT3 activation by targeting SHP-1
Jung-Chen Su, Chuan-Hsun Chang, Szu-Hsien Wu & Chung-Wai Shiau
Pages: 1248-1255
Published online: 28 Sep 2018
AbstractforNovel imidazopyridine suppresses STAT3 activation by targeting SHP-1 | Full Text | References | PDF (1.2 MB)
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Article
Design, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase
Bo Ram Kim, Ji-Young Park, Hyung Jae Jeong, Hyung-Jun Kwon, Su-Jin Park, In-Chul Lee, Young Bae Ryu & Woo Song Lee
Pages: 1256-1265
Published online: 21 Aug 2018
AbstractforDesign, synthesis, and evaluation of curcumin analogues as potential inhibitors of bacterial sialidase | Full Text | References | PDF (1.2 MB) | Supplemental
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Ethenesulfonyl fluoride derivatives as telomerase inhibitors: structure-based design, SAR, and anticancer evaluation in vitro
Xing Chen, Gao-Feng Zha, Jie Quan Wang & Xin-Hua Liu
Pages: 1266-1270
Published online: 24 Aug 2018
AbstractforEthenesulfonyl fluoride derivatives as telomerase inhibitors: structure-based design, SAR, and anticancer evaluation in vitro | Full Text | References | PDF (961.9 KB)
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Article
Synthesis and structure–activity relationships of 2- and/or 4-halogenated 13β- and 13α-estrone derivatives as enzyme inhibitors of estrogen biosynthesis
Ildikó Bacsa, Bianka Edina Herman, Rebeka Jójárt, Kevin Stefán Herman, János Wölfling, Gyula Schneider, Mónika Varga, Csaba Tömböly, Tea Lanišnik Rižner, Mihály Szécsi & Erzsébet Mernyák
Pages: 1271-1282
Published online: 19 Sep 2018
AbstractforSynthesis and structure–activity relationships of 2- and/or 4-halogenated 13β- and 13α-estrone derivatives as enzyme inhibitors of estrogen biosynthesis | Full Text | References | PDF (3.2 MB) | Supplemental
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Article
Identification of flavonolignans from Silybum marianum seeds as allosteric protein tyrosine phosphatase 1B inhibitors
Ningbo Qin, Tatsunori Sasaki, Wei Li, Jian Wang, Xiangyu Zhang, Dahong Li, Zhanlin Li, Maosheng Cheng, Huiming Hua & Kazuo Koike
Pages: 1283-1291
Published online: 30 Aug 2018
AbstractforIdentification of flavonolignans from Silybum marianum seeds as allosteric protein tyrosine phosphatase 1B inhibitors | Full Text | References | PDF (1.8 MB)
  • 1890 Views
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Article
Myeloperoxidase, a possible biomarker for the early diagnosis of cardiac diastolic dysfunction with preserved ejection fraction
Bogdan Ioan Coculescu, Gabi Valeriu Dincă, Constantin Bălăeţ, Gheorghe Manole, Maria Bălăeţ & Cristina Mariana Stocheci
Pages: 1292-1298
Published online: 31 Aug 2018
AbstractforMyeloperoxidase, a possible biomarker for the early diagnosis of cardiac diastolic dysfunction with preserved ejection fraction | Full Text | References | PDF (776.2 KB)
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Article
Novel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group acting as human carbonic anhydrase IX inhibitors
Özlen Güzel-Akdemir, Andrea Angeli, Kübra Demir, Claudiu T. Supuran & Atilla Akdemir
Pages: 1299-1308
Published online: 24 Sep 2018
AbstractforNovel thiazolidinone-containing compounds, without the well-known sulphonamide zinc-binding group acting as human carbonic anhydrase IX inhibitors | Full Text | References | PDF (1.5 MB)
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Article
Metformin and its sulphonamide derivative simultaneously potentiateanti-cholinesterase activity of donepezil and inhibit beta-amyloid aggregation
Magdalena Markowicz-Piasecka, Kristiina M. Huttunen & Joanna Sikora
Pages: 1309-1322
Published online: 24 Sep 2018
AbstractforMetformin and its sulphonamide derivative simultaneously potentiateanti-cholinesterase activity of donepezil and inhibit beta-amyloid aggregation | Full Text | References | PDF (2 MB) | Supplemental
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Article
Synthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA
Andrea Bistrović, Luka Krstulović, Ivana Stolić, Domagoj Drenjančević, Jasminka Talapko, Martin C. Taylor, John M. Kelly, Miroslav Bajić & Silvana Raić-Malić
Pages: 1323-1334
Published online: 31 Aug 2018
AbstractforSynthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA | Full Text | References | PDF (1.8 MB) | Supplemental
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Article
Rapidly screening of α-glucosidase inhibitors from Dioscorea opposita Thunb. peel based on rGO@Fe3O4 nanocomposites microreactor
Songsong Zhang, Beibei Qiu, Jinhua Zhu, Weiping Hu, Fanyi Ma, M. Z. H. Khan & Xiuhua Liu
Pages: 1335-1342
Published online: 19 Sep 2018
AbstractforRapidly screening of α-glucosidase inhibitors from Dioscorea opposita Thunb. peel based on rGO@Fe3O4 nanocomposites microreactor | Full Text | References | PDF (1.7 MB)
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Article
Inhibition of O-acetylserine sulfhydrylase by fluoroalanine derivatives
Nina Franko, Konstantinos Grammatoglou, Barbara Campanini, Gabriele Costantino, Aigars Jirgensons & Andrea Mozzarelli
Pages: 1343-1351
Published online: 24 Sep 2018
AbstractforInhibition of O-acetylserine sulfhydrylase by fluoroalanine derivatives | Full Text | References | PDF (2.3 MB) | Supplemental
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Article
Synthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents
Burcu Çalışkan, Esra Sinoplu, Kübra İbiş, Ece Akhan Güzelcan, Rengül Çetin Atalay & Erden Banoglu
Pages: 1352-1361
Published online: 24 Sep 2018
AbstractforSynthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents | Full Text | References | PDF (2.3 MB) | Supplemental
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Article
Coptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process
Cailan Li, Ping Huang, Kambo Wong, Yifei Xu, Lihua Tan, Hanbin Chen, Qiang Lu, Chaodan Luo, Chunlai Tam, Lixiang Zhu, Ziren Su & Jianhui Xie
Pages: 1362-1375
Published online: 07 Sep 2018
AbstractforCoptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process | Full Text | References | PDF (2.6 MB)
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Synthesis and biological evaluation of dithiocarbamate esters of parthenolide as potential anti-acute myelogenous leukaemia agents
Yahui Ding, Zhongjin Yang, Weizhi Ge, Beijia Kuang, Junqing Xu, Juan Yang, Yue Chen & Quan Zhang
Pages: 1376-1391
Published online: 13 Sep 2018
AbstractforSynthesis and biological evaluation of dithiocarbamate esters of parthenolide as potential anti-acute myelogenous leukaemia agents | Full Text | References | PDF (4.4 MB) | Supplemental
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The new H2S-releasing compound ACS94 exerts protective effects through the modulation of thiol homoeostasis
Daniela Giustarini, Valerio Tazzari, Ivan Bassanini, Ranieri Rossi & Anna Sparatore
Pages: 1392-1404
Published online: 03 Sep 2018
AbstractforThe new H2S-releasing compound ACS94 exerts protective effects through the modulation of thiol homoeostasis | Full Text | References | PDF (2.4 MB)
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In the quest for new targets for pathogen eradication: the adenylosuccinate synthetase from the bacterium Helicobacter pylori
Ante Bubić, Natalia Mrnjavac, Igor Stuparević, Marta Łyczek, Beata Wielgus-Kutrowska, Agnieszka Bzowska, Marija Luić & Ivana Leščić Ašler
Pages: 1405-1414
Published online: 07 Sep 2018
AbstractforIn the quest for new targets for pathogen eradication: the adenylosuccinate synthetase from the bacterium Helicobacter pylori | Full Text | References | PDF (1.4 MB) | Supplemental
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Novel group of tyrosyl-DNA-phosphodiesterase 1 inhibitors based on disaccharide nucleosides as drug prototypes for anti-cancer therapy
Anastasia O. Komarova, Mikhail S. Drenichev, Nadezhda S. Dyrkheeva, Irina V. Kulikova, Vladimir E. Oslovsky, Olga D. Zakharova, Alexandra L. Zakharenko, Sergey N. Mikhailov & Olga I. Lavrik
Pages: 1415-1429
Published online: 07 Sep 2018
AbstractforNovel group of tyrosyl-DNA-phosphodiesterase 1 inhibitors based on disaccharide nucleosides as drug prototypes for anti-cancer therapy | Full Text | References | PDF (4.2 MB) | Supplemental
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Target-based drug discovery through inversion of quantitative structure-drug-property relationships and molecular simulation: CA IX-sulphonamide complexes
Petar Žuvela, J. Jay Liu, Myunggi Yi, Paweł P. Pomastowski, Gulyaim Sagandykova, Mariusz Belka, Jonathan David, Tomasz Bączek, Krzysztof Szafrański, Beata Żołnowska, Jarosław Sławiński, Claudiu T. Supuran, Ming Wah Wong & Bogusław Buszewski
Pages: 1430-1443
Published online: 17 Sep 2018
AbstractforTarget-based drug discovery through inversion of quantitative structure-drug-property relationships and molecular simulation: CA IX-sulphonamide complexes | Full Text | References | PDF (3 MB) | Supplemental
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Discovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand–based drug design
Joana Magalhães, Nina Franko, Giannamaria Annunziato, Martin Welch, Stephen K. Dolan, Agostino Bruno, Andrea Mozzarelli, Stefano Armao, Aigars Jirgensons, Marco Pieroni, Gabriele Costantino & Barbara Campanini
Pages: 1444-1452
Published online: 17 Sep 2018
AbstractforDiscovery of novel fragments inhibiting O-acetylserine sulphhydrylase by combining scaffold hopping and ligand–based drug design | Full Text | References | PDF (1.3 MB)
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Steroids interfere with human carbonic anhydrase activity by using alternative binding mechanisms
Alessio Nocentini, Alessandro Bonardi, Paola Gratteri, Bruno Cerra, Antimo Gioiello & Claudiu T. Supuran
Pages: 1453-1459
Published online: 17 Sep 2018
AbstractforSteroids interfere with human carbonic anhydrase activity by using alternative binding mechanisms | Full Text | References | PDF (1.6 MB)
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Original Article

Article
Synthesis and biological evaluation of pyrrolidine-based T-type calcium channel inhibitors for the treatment of neuropathic pain
Hak Kyun Yang, Woo Seung Son, Keon Seung Lim, Gun Hee Kim, Eun Jeong Lim, Changdev G. Gadhe, Jae Yeol Lee, Kyu-Sung Jeong, Sang Min Lim & Ae Nim Pae
Pages: 1460-1471
Published online: 20 Sep 2018
AbstractforSynthesis and biological evaluation of pyrrolidine-based T-type calcium channel inhibitors for the treatment of neuropathic pain | Full Text | References | PDF (1.9 MB) | Supplemental
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Articles

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Design, synthesis, and screening of ortho-amino thiophene carboxamide derivatives on hepatocellular carcinomaas VEGFR-2Inhibitors
Mohammed K. AbdElhameid, Madlen B. Labib, Ahmed T. Negmeldin, Muhammad Al-Shorbagy & Manal R. Mohammed
Pages: 1472-1493
Published online: 07 Sep 2018
AbstractforDesign, synthesis, and screening of ortho-amino thiophene carboxamide derivatives on hepatocellular carcinomaas VEGFR-2Inhibitors | Full Text | References | PDF (3.5 MB) | Supplemental
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Research Paper

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Inhibition of p38 mitogen-activated protein kinase exerts a hypoglycemic effect by improving β cell function via inhibition of β cell apoptosis in db/db mice
Xiaowei Wei, Nan Gu, Nan Feng, Xiaohui Guo & Xiaowei Ma
Pages: 1494-1500
Published online: 04 Oct 2018
AbstractforInhibition of p38 mitogen-activated protein kinase exerts a hypoglycemic effect by improving β cell function via inhibition of β cell apoptosis in db/db mice | Full Text | References | PDF (1.6 MB) | Supplemental
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RESEARCH PAPER

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Hyperbaric oxygen therapy ameliorates osteonecrosis in patients by modulating inflammation and oxidative stress
Gerardo Bosco, Giuliano Vezzani, Simona Mrakic Sposta, Alex Rizzato, Garrett Enten, Abdullah Abou-samra, Sandro Malacrida, Silvia Quartesan, Alessandra Vezzoli & Enrico Camporesi
Pages: 1501-1505
Published online: 01 Oct 2018
AbstractforHyperbaric oxygen therapy ameliorates osteonecrosis in patients by modulating inflammation and oxidative stress | Full Text | References | PDF (700.1 KB)
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Short Communication

Rapid Communication
Design, synthesis and biological evaluation of tricyclic pyrazolo[1,5-c][1,3]benzoxazin-5(5H)-one scaffolds as selective BuChE inhibitors
Guo-Liang Qiu, Shao-Sheng He, Shi-Chao Chen, Bo Li, Hui-Hui Wu, Jing Zhang & Wen-Jian Tang
Pages: 1506-1515
Published online: 04 Oct 2018
AbstractforDesign, synthesis and biological evaluation of tricyclic pyrazolo[1,5-c][1,3]benzoxazin-5(5H)-one scaffolds as selective BuChE inhibitors | Full Text | References | PDF (2.1 MB) | Supplemental
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Benzofuran–appended 4-aminoquinazoline hybrids as epidermal growth factor receptor tyrosine kinase inhibitors: synthesis, biological evaluation and molecular docking studies
Malose J. Mphahlele, Marole M. Maluleka, Abimbola Aro, Lyndy J. McGaw & Yee Siew Choong
Pages: 1516-1528
Published online: 02 Oct 2018
AbstractforBenzofuran–appended 4-aminoquinazoline hybrids as epidermal growth factor receptor tyrosine kinase inhibitors: synthesis, biological evaluation and molecular docking studies | Full Text | References | PDF (2.3 MB) | Supplemental
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Pharmacophore-based discovery of 2-(phenylamino)aceto-hydrazides as potent eosinophil peroxidase (EPO) inhibitors
Daniela Schuster, Martina Zederbauer, Thierry Langer, Andreas Kubin & Paul G. Furtmüller
Pages: 1529-1536
Published online: 04 Oct 2018
AbstractforPharmacophore-based discovery of 2-(phenylamino)aceto-hydrazides as potent eosinophil peroxidase (EPO) inhibitors | Full Text | References | PDF (1.7 MB) | Supplemental
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Discovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases
Giannamaria Annunziato, Laura Giovati, Andrea Angeli, Marialaura Pavone, Sonia Del Prete, Marco Pieroni, Clemente Capasso, Agostino Bruno, Stefania Conti, Walter Magliani, Claudiu T. Supuran & Gabriele Costantino
Pages: 1537-1544
Published online: 04 Oct 2018
AbstractforDiscovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases | Full Text | References | PDF (1.5 MB)
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Design, synthesis, and biological evaluation of novel iso-flavones derivatives as H3R antagonists
Jian Xin, Min Hu, Qian Liu, Tian Tai Zhang, Dong Mei Wang & Song Wu
Pages: 1545-1553
Published online: 07 Oct 2018
AbstractforDesign, synthesis, and biological evaluation of novel iso-flavones derivatives as H3R antagonists | Full Text | References | PDF (1.6 MB)
  • 992 Views
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Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents
Ya-Bing Xin, Jia-Jun Li, Hong-Jian Zhang, Jun Ma, Xin Liu, Guo-Hua Gong & Yu-Shun Tian
Pages: 1554-1564
Published online: 23 Sep 2018
AbstractforSynthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents | Full Text | References | PDF (2.3 MB) | Supplemental
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Carbonic anhydrase inhibition with a series of novel benzenesulfonamide-triazole conjugates
Marwa G. El-Gazzar, Nessma H. Nafie, Alessio Nocentini, Mostafa M. Ghorab, Helmi I. Heiba & Claudiu T. Supuran
Pages: 1565-1574
Published online: 02 Oct 2018
AbstractforCarbonic anhydrase inhibition with a series of novel benzenesulfonamide-triazole conjugates | Full Text | References | PDF (1.1 MB)
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Discovery of novel 1,3-diaryltriazene sulfonamides as carbonic anhydrase I, II, VII, and IX inhibitors
Suleyman Akocak, Nabih Lolak, Silvia Bua & Claudiu T. Supuran
Pages: 1575-1580
Published online: 09 Oct 2018
AbstractforDiscovery of novel 1,3-diaryltriazene sulfonamides as carbonic anhydrase I, II, VII, and IX inhibitors | Full Text | References | PDF (1.3 MB)
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