Identification of pyrazolo [1, 5-a] pyrimidine-3-carboxylates as B-Raf kinase inhibitors

…, E Frommer, S Kim, K Collins, D Wojciechowicz…

Index: Gopalsamy, Ariamala; Ciszewski, Greg; Hu, Yongbo; Lee, Frederick; Feldberg, Larry; Frommer, Eileen; Kim, Steven; Collins, Karen; Wojciechowicz, Donald; Mallon, Robert Bioorganic and Medicinal Chemistry Letters, 2009 ,  vol. 19,  # 10  p. 2735 - 2738

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Citation Number: 24

Abstract

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.