Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase.
Bioorganic & Medicinal Chemistry Letters(2013)
摘要
This Letter details the synthesis and evaluation of imidazo[4,5-b]pyridines as inhibitors of B-Raf kinase. These compounds bind in a DFG-in, αC-helix out conformation of B-Raf, which is a binding mode associated with significant kinase selectivity. Structure–activity relationship studies involved optimization of the ATP-cleft binding region of these molecules, and led to compound 23, an inhibitor with excellent enzyme/cell potency, and kinase selectivity.
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关键词
B-Raf,Imidazopyridine,Scaffold hopping,DFG-in,αC-helix out
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