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Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors |
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| Authors: | Packard Garrick K Papa Patrick Riggs Jennifer R Erdman Paul Tehrani Lida Robinson Dale Harris Roy Shevlin Graziella Perrin-Ninkovic Sophie Hilgraf Robert McCarrick Margaret A Tran Tam Fleming Yuedi Bai April Richardson Samantha Katz Jason Tang Yang Leisten Jim Moghaddam Mehran Cathers Brian Zhu Dan Sakata Steven |
| Institution: | Celgene Corporation, San Diego, 4550 Towne Centre Ct, San Diego, CA 92121, United States. gkpackardca@gmail.com |
| Abstract: | The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described. |
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