Flipped out: Structure-guided design of selective pyrazolylpyrrole ERK inhibitors

Alex M. Aronov, Christopher Baker, Guy W. Bemis, Jingrong Cao, Guanjing Chen, Pamella J. Ford, Ursula A. Germann, Jeremy Green, Michael R. Hale, Marc Jacobs, James W. Janetka, Francois Maltais, Gabriel Martinez-Botella, Mark N. Namchuk, Judy Straub, Qing Tang, Xiaoling Xie

Research output: Contribution to journalArticlepeer-review

98 Scopus citations

Abstract

The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.

Original languageEnglish
Pages (from-to)1280-1287
Number of pages8
JournalJournal of Medicinal Chemistry
Volume50
Issue number6
DOIs
StatePublished - Mar 22 2007

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