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

ABSTRACT: 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.

SUBMITTER: Bryan MC 

PROVIDER: S-EPMC4716594 | biostudies-literature | 2016 Jan

REPOSITORIES: biostudies-literature

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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. ...[more]

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