Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors

被引：42

作者：

Liu, Lee Tai

Yuan, Ta-Tung

Liu, Hung-Huang

Chen, Shyh-Fong

Wu, Ying-Ta

机构：

[1] Dev Ctr Biotechnol, Taipei, Taiwan

[2] Genomics Res Ctr, Taipei, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期

关键词：

EGFR kinase inhibitor; alkynyl-substituted; 4-anifnoquinazoline;

D O I：

10.1016/j.bmcl.2007.08.061

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of C-6 or C-3 ' alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC50 of 14 nM. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6373 / 6377

页数：5

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