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

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

Bioorganic & medicinal chemistry letters (2009-09-19)

Chuansheng Niu, Diane H Boschelli, L Nathan Tumey, Niala Bhagirath, Joan Subrath, Jaechul Shim, Yan Wang, Biqi Wu, Clark Eid, Julie Lee, Xiaoke Yang, Agnes Brennan, Divya Chaudhary

PMID19762237

RÉSUMÉ

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.