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Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.

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 EC(50) of less than 1 nM against wild-type Bcr-Abl and an EC(50) of 10 nM against T315I mutant but is broadly active against a number of other kinases.

SUBMITTER: Deng X

PROVIDER: S-EPMC2901992 | biostudies-literature | 2010 Jul

REPOSITORIES: biostudies-literature

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Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.

Deng Xianming X Lim Sang Min SM Zhang Jianming J Gray Nathanael S NS

Bioorganic & medicinal chemistry letters 20100519 14

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 EC(50) of less than 1 nM against wild-type Bcr-Abl and an EC(50) of 10 nM against T315I mutant but is broadly active against a number of other kinases. ...[more]

PMID: 20541934

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