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Article

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

Bioorganic & medicinal chemistry letters - 15 Aug 2012

Choi Hwan Geun, Zhang Jianming, Weisberg Ellen, Griffin James D, Sim Taebo, Gray Nathanael S

Abstract excerpt

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.

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Identifiers

PMID: 22819762
DOI: 10.1016/j.bmcl.2012.06.036
PMCID: PMC3415686

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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