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

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.

Graphical abstractIdentification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase Inhibitor and the SAR requirements are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide