1018143-51-5Relevant articles and documents
Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-RafV600E kinase with favorable physicochemical and pharmacokinetic properties
Ren, Li,Laird, Ellen R.,Buckmelter, Alex J.,Dinkel, Victoria,Gloor, Susan L.,Grina, Jonas,Newhouse, Brad,Rasor, Kevin,Hastings, Gregg,Gradl, Stefan N.,Rudolph, Joachim
scheme or table, p. 1165 - 1168 (2012/03/11)
Herein we describe a novel series of ATP competitive B-Raf inhibitors based on the pyrazolo[1,5-a]pyrimidine scaffold. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization led to the identification of compound 17, a potent, selective and orally available agent with improved physicochemical and pharmacokinetic properties.