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

详细信息    查看全文

• 作者：Marian C. Bryan ; Daniel J. Burdick ; Bryan K. Chan ; Yuan Chen ; Saundra Clausen ; Jennafer Dotson ; Charles Eigenbrot ; Richard Elliott ; Emily J. Hanan ; Robert Heald ; Philip Jackson ; Hank La ; Michael Lainchbury ; Shiva Malek ; Sam E. Mann ; Hans E. Purkey ; Gabriele Schaefer ; Stephen Schmidt ; Eileen Seward ; Steve Sideris ; Shumei Wang ; Ivana Yen ; Christine Yu ; Timothy P. Heffron
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：January 14, 2016
• 年：2016
• 卷：7
• 期：1
• 页码：100-104
• 全文大小：382K
• ISSN：1948-5875

文摘

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.