2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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

Authors:	Nathan Tumey L Boschelli Diane H Lee Julie Chaudhary Divya

Affiliation:	^aWyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA;^bWyeth Research, Inflammation, 200 Cambridge Park Drive, Cambridge, MA 12140, USA

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.

Keywords:	Kinase PKC PKCθ PKCδ Indole Inflammation T cell Thienopyridine Cyano Nitrile
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