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Discovery of thieno[2,3-c]pyridines as potent COT inhibitors |
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| Authors: | George Dawn Friedman Michael Allen Hamish Argiriadi Maria Barberis Claude Bischoff Agnieszka Clabbers Anca Cusack Kevin Dixon Richard Fix-Stenzel Shannon Gordon Thomas Janssen Bernd Jia Yong Moskey Maria Quinn Christopher Salmeron Jose-Andres Wishart Neil Woller Kevin Yu Zhengtian |
| Institution: | Abbott Bioresearch Center, 381 Plantation Street, Worcester, MA 01605, USA. dawn.george@abbott.com |
| Abstract: | Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno2,3-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. |
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