Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents

被引：35

作者：

An, Weiteng ^{[1
]}

Wang, Wei ^{[1
]}

Yu, Ting ^{[1
]}

Zhang, Yongliang ^{[1
]}

Miao, Zehong ^{[1
]}

Meng, Tao ^{[1
]}

Shen, Jingkang ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 112卷

基金：

中国国家自然科学基金;

关键词：

Anticancer agents; Tubulin inhibitor; Intra-molecular hydrogen bonding; Colchicine binding site; 3-COMPONENT CONDENSATION; COMBINATORIAL SYNTHESIS; ANTICANCER DRUGS; INHIBITORS; COLCHICINE; PYRAZINES; BINDING;

D O I：

10.1016/j.ejmech.2016.02.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-aryl-imidazo-pyridines/pyrazines derivatives has been designed, synthesized and evaluated for their biological activities. Among them, several investigated compounds (1a, 3b and 3d) displayed potent antiproliferative activity against HeLa cell, and also displayed comparable tubulin polymerization inhibitory activity to colchicine. These studies provided a new molecular scaffold for the further development of antitumor agents that target tubulin. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：367 / 372

页数：6

共 24 条

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