Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 4, Pages 1976-1991Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm501921k
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Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, (S)-14k was selected for further preclinical evaluation.
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