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Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors. 2009
Ariamala Gopalsamy, and
Greg Ciszewski, and
Yongbo Hu, and
Frederick Lee, and
Larry Feldberg, and
Eileen Frommer, and
Steven Kim, and
Karen Collins, and
Donald Wojciechowicz, and
Robert Mallon
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. gopalsa@wyeth.com
B-Raf kinase plays a critical role in the Raf-MEK-ERK signaling pathway and inhibitors of B-Raf could be used in the treatment of melanomas, colorectal cancer, and other Ras related human cancers. We have identified novel small molecule pyrazolo[1,5-a]pyrimidine derivatives as B-Raf kinase inhibitors. Structure-activity relationship was generated for various regions of the scaffold to improve the biochemical profile.
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