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Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors. 2012
Garrick K Packard, and
Patrick Papa, and
Jennifer R Riggs, and
Paul Erdman, and
Lida Tehrani, and
Dale Robinson, and
Roy Harris, and
Graziella Shevlin, and
Sophie Perrin-Ninkovic, and
Robert Hilgraf, and
Margaret A McCarrick, and
Tam Tran, and
Yuedi Fleming, and
April Bai, and
Samantha Richardson, and
Jason Katz, and
Yang Tang, and
Jim Leisten, and
Mehran Moghaddam, and
Brian Cathers, and
Dan Zhu, and
Steven Sakata
Celgene Corporation, San Diego, 4550 Towne Centre Ct, San Diego, CA 92121, United States. gkpackardca@gmail.com
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-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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