Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases
- Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases
- 최환근; Jianming Zhang; Ellen Weisberg; James D. Griffin; 심태보; Nathanael S. Gray
- T315I Bcr-Abl; Kinase inhibitor; Gatekeeper mutant; Type II inhibitor; Thiazolo[5,4-b]pyridine
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 22, NO 16, 5297-5302
- 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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