950739-24-9Relevant articles and documents
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors
Berger, Dan M.,Torres, Nancy,Dutia, Minu,Powell, Dennis,Ciszewski, Greg,Gopalsamy, Ariamala,Levin, Jeremy I.,Kim, Kyung-Hee,Xu, Weixin,Wilhelm, James,Hu, YongBo,Collins, Karen,Feldberg, Larry,Kim, Steven,Frommer, Eileen,Wojciechowicz, Donald,Mallon, Robert
scheme or table, p. 6519 - 6523 (2010/05/18)
As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallography studies revealed that one of the more potent inhibitors (10n) bound to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.
