Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 1, Pages 100-104Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00428
Keywords
Mutant EGFR; noncovalent; pyridone; T790M
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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.
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