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

…, DH Boschelli, J Lee, D Chaudhary

Index: Nathan Tumey; Boschelli, Diane H.; Lee, Julie; Chaudhary, Divya Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4420 - 4423

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Citation Number: 40

Abstract

A series of 2-alkenyl thieno [2, 3-b] pyridine inhibitors of PKCθ were synthesized as potential inflammatory modulators. This series led to the discovery of 2-alkenyl amides, which are exceptionally potent and selective inhibitors of PKCθ. Compound 8 has an IC50 of 3.8 nM against PKCθ and shows excellent selectivity over a variety of PKC isoforms.