Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
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ABSTRACT:
SUBMITTER: Bryan MC
PROVIDER: S-EPMC4716594 | biostudies-literature | 2016 Jan
REPOSITORIES: biostudies-literature
Publications
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Bryan Marian C MC Burdick Daniel J DJ Chan Bryan K BK Chen Yuan Y Clausen Saundra S Dotson Jennafer J Eigenbrot Charles C Elliott Richard R Hanan Emily J EJ Heald Robert R Jackson Philip P La Hank H Lainchbury Michael M Malek Shiva S Mann Sam E SE Purkey Hans E HE Schaefer Gabriele G Schmidt Stephen S Seward Eileen E Sideris Steve S Wang Shumei S Yen Ivana I Yu Christine C Heffron Timothy P TP
ACS medicinal chemistry letters 20151217 1
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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