Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

ACS medicinal chemistry letters（2016）

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摘要

The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with high levels of selectivity over wtEGFR and the broader kinome is described herein.

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关键词

Mutant EGFR,T790M,noncovalent,pyridone

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