2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta |
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| Authors: | Nathan Tumey L Boschelli Diane H Lee Julie Chaudhary Divya |
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| Institution: | 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 |
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| Abstract: | A series of 2-alkenyl thieno2,3-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. |
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| Keywords: | Kinase PKC PKCθ PKCδ Indole Inflammation T cell Thienopyridine Cyano Nitrile |
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