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  • Title: 2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
    Author: Nathan Tumey L, Boschelli DH, Lee J, Chaudhary D.
    Journal: Bioorg Med Chem Lett; 2008 Aug 01; 18(15):4420-3. PubMed ID: 18606543.
    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.
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