Discovery of highly potent and selective type I B-Raf kinase inhibitors

A series of pyrazolo[1,5-α]pyrimidine analogs has been prepared and found to be potent and selective B-Raf inhibitors. Molecular modeling suggests they bind to the active conformation of the enzyme.

Graphical abstractA series of pyrazolo[1,5-α]pyrimidine analogs has been prepared and found to be extremely potent and selective B-Raf inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide