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Bioorg Med Chem Lett. 2008 Aug 1;18(15):4420-3. doi: 10.1016/j.bmcl.2008.06.040. Epub 2008 Jun 18.

2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.

Author information

1
Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA. nathantumey@yahoo.com

Abstract

A series of 2-alkenyl thieno[2,3-b]pyridine inhibitors of PKCtheta were synthesized as potential inflammatory modulators. This series led to the discovery of 2-alkenyl amides, which are exceptionally potent and selective inhibitors of PKCtheta. Compound 8 has an IC(50) of 3.8nM against PKCtheta and shows excellent selectivity over a variety of PKC isoforms.

PMID:
18606543
DOI:
10.1016/j.bmcl.2008.06.040
[Indexed for MEDLINE]

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