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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7381-7. doi: 10.1016/j.bmcl.2012.10.066. Epub 2012 Oct 24.

Discovery of a novel series of 4-quinolone JNK inhibitors.

Author information

1
Department of Medicinal Chemistry, Roche Palo Alto, Palo Alto, CA 94304, USA. leyi.gong@sri.com

Abstract

A novel series of highly selective JNK inhibitors based on the 4-quinolone scaffold was designed and synthesized. Structure based drug design was utilized to guide the compound design as well as improvements in the physicochemical properties of the series. Compound (13c) has an IC(50) of 62/170 nM for JNK1/2, excellent kinase selectivity and impressive efficacy in a rodent asthma model.

PMID:
23142618
DOI:
10.1016/j.bmcl.2012.10.066
[Indexed for MEDLINE]

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