Flipped Out: Structure-Guided Design of Selective Pyrazolylpyrrole ERK Inhibitors
Journal of Medicinal Chemistry2007Vol. 50(6), pp. 1280–1287
Citations Over TimeTop 10% of 2007 papers
Alex M. Aronov, Christopher Baker, Guy W. Bemis, Jingrong Cao, Guanjing Chen, Pamella J. Ford, Ursula A. Germann, Jeremy Green, Michael Hale, Marc Jacobs, James W. Janetka, François Maltais, Gabriel Martínez-Botella, Mark Namchuk, Judy Straub, Qing Tang, Xiaoling Xie
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.
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