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.

Graphical abstractA 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 full-size imageDownload as PowerPoint slide