Broad spectrum alkynyl inhibitors of T315I Bcr-Abl

X Deng, SM Lim, J Zhang, NS Gray

Index: Deng, Xianming; Lim, Sang Min; Zhang, Jianming; Gray, Nathanael S. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 14 p. 4196 - 4200

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Citation Number: 22

Abstract

A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC50 of less than 1nM against wild-type Bcr-Abl and an EC50 of 10nM against T315I mutant but is broadly active against a number of other kinases.