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 IC 50 of 3.8 nM against PKCθ and shows excellent selectivity over a variety of PKC isoforms.
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