Literature DB >> 20947362

Synthesis, biological evaluation, and molecular docking studies of 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety as potential antitumor agents.

Qing-Zhong Zheng1, Xiao-Min Zhang, Ying Xu, Kui Cheng, Qing-Cai Jiao, Hai-Liang Zhu.   

Abstract

A series of new 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety were synthesized. Antiproliferative assay results indicated that compounds 6o and 6u exhibited the most potent activity against gastric cancer cell SGC-7901, which was more potent than the positive control. Especially, compound 6o exhibited significant telomerase inhibitory activity (IC(50)=2.3±0.07μM), which was comparable to the positive control ethidium bromide. Docking simulation was performed to position compound 6o into the active site of telomerase (3DU6) to determine the probable binding model.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20947362     DOI: 10.1016/j.bmc.2010.09.051

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  6 in total

1.  Rapid, Microwave Accelerated Synthesis of [1,2,4]Triazolo[3,4-b][1,3,4]oxadiazoles from 4-Acylamino-1,2,4-Triazoles.

Authors:  Stesphanie L Breunig; Margaret E Olson; Daniel A Harki
Journal:  Tetrahedron Lett       Date:  2016-07-29       Impact factor: 2.415

2.  Ethenesulfonyl fluoride derivatives as telomerase inhibitors: structure-based design, SAR, and anticancer evaluation in vitro.

Authors:  Xing Chen; Gao-Feng Zha; Jie Quan Wang; Xin-Hua Liu
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

3.  Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety.

Authors:  Xu Han; Yun Long Yu; Duo Ma; Zhao Yan Zhang; Xin Hua Liu
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

4.  Synthesis and In Vitro Biological Evaluation of 1,3,4-Oxadiazol-2(3H)-one and Tetrahydropyridazine-3,6-dione Derivatives of Fatty Acids.

Authors:  Mohammad F Hassan; Abdul Rauf; Asif Sherwani; Mohammad Owais
Journal:  Sci Pharm       Date:  2015-06-09

Review 5.  Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds.

Authors:  Alessandra Benassi; Filippo Doria; Valentina Pirota
Journal:  Int J Mol Sci       Date:  2020-11-18       Impact factor: 5.923

6.  In Silico Design, Synthesis, and Biological Evaluation of Anticancer Arylsulfonamide Endowed with Anti-Telomerase Activity.

Authors:  Giulia Culletta; Mario Allegra; Anna Maria Almerico; Ignazio Restivo; Marco Tutone
Journal:  Pharmaceuticals (Basel)       Date:  2022-01-10
  6 in total

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