Discovery of thieno[2,3-c]pyridines as potent COT inhibitors

Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with improved enzyme potency and cellular activity are disclosed.

A series of thieno[2,3-c]pyridines were identified as potent inhibitors of COT kinase activity. Structural modifications exploring SAR resulted in the identification of inhibitors with improved enzyme potency and cellular activity.Figure optionsDownload as PowerPoint slide