Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors

…, CF Zhou, J Chen, PG Liu, KR Wang, WJ Mao…

Index: Lv, Peng-Cheng; Zhou, Chang-Fang; Chen, Jin; Liu, Peng-Gang; Wang, Kai-Rui; Mao, Wen-Jun; Li, Huan-Qiu; Yang, Ying; Xiong, Jing; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 1 p. 314 - 319

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Citation Number: 68

Abstract

Two series of thiazolidinone derivatives designing for potential EGFR and HER-2 kinase inhibitors have been discovered. Some of them exhibited significant EGFR and HER-2 inhibitory activity. Compound 2-(2-(5-bromo-2-hydroxybenzylidene) hydrazinyl) thiazol-4 (5H)-one (12) displayed the most potent inhibitory activity (IC50= 0.09 μM for EGFR and IC50= 0.42 μM for HER-2), comparable to the positive control erlotinib. Docking simulation ...