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First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors

, : First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors. Bioorganic & Medicinal Chemistry Letters 19(20): 5829-5832

A series of 5-vinyl-3-pyridinecarbonitriles were synthesized and evaluated as PKCtheta inhibitors. The systematic optimization of 4-[(4-methyl-1H-indol-5-yl)amino]-5-[(E)-2-phenylvinyl]-3-pyridinecarbonitrile 3 resulted in the identification of compound 23e as a potent PKCtheta inhibitor with good selectivity over PKCdelta.


PMID: 19762237

DOI: 10.1016/j.bmcl.2009.08.086

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