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Bioorg Med Chem Lett. 2009 Dec 1;19(23):6575-7. doi: 10.1016/j.bmcl.2009.10.031. Epub 2009 Oct 13.

Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.

Author information

1
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA. shimj@wyeth.com

Abstract

A series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles were prepared and evaluated as PKCtheta inhibitors. Optimization resulted in the identification of compound 15 with an IC(50) value 0.44 nM for the inhibition of PKCtheta with 150-fold selectivity over PKCdelta.

PMID:
19854645
DOI:
10.1016/j.bmcl.2009.10.031
[Indexed for MEDLINE]

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