Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373087 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A series of 5-vinyl-3-pyridinecarbonitriles were synthesized and evaluated as PKCθ 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 PKCθ inhibitor with good selectivity over PKCδ.
Graphical abstractThe synthesis of a series of 5-vinyl-3-pyridinecarbonitriles resulted in a potent PKCθ inhibitor 23e, which had an IC50 value of 4.7 nM for the inhibition of PKCθ with 11-fold selectivity over PKCδ.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,