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Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.

ABSTRACT: HG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and 'gatekeeper' mutant T315I- Bcr-Abl. Here we report on the 'hybrid design' concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors.

SUBMITTER: Choi HG 

PROVIDER: S-EPMC3415686 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature

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Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.

Choi Hwan Geun HG   Zhang Jianming J   Weisberg Ellen E   Griffin James D JD   Sim Taebo T   Gray Nathanael S NS  

Bioorganic & medicinal chemistry letters 20120623 16

HG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and 'gatekeeper' mutant T315I- Bcr-Abl. Here we report on the 'hybrid design' concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors. ...[more]

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