First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.

ID: ALA1156064

Journal: Bioorg Med Chem Lett

Title: First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.

Authors: Niu C, Boschelli DH, Tumey LN, Bhagirath N, Subrath J, Shim J, Wang Y, Wu B, Eid C, Lee J, Yang X, Brennan A, Chaudhary D.

Abstract: 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.

CiteXplore: 19762237

DOI: 10.1016/j.bmcl.2009.08.086

Patent ID: ┄