Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors.

Abstract 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.