1191385-20-2Relevant articles and documents
Selective inhibitors of the mutant B-Raf pathway: Discovery of a potent and orally bioavailable aminoisoquinoline
Smith, Adrian L.,DeMorin, Frenel F.,Paras, Nick A.,Huang, Qi,Petkus, Jeffrey K.,Doherty, Elizabeth M.,Nixey, Thomas,Kim, Joseph L.,Whittington, Douglas A.,Epstein, Linda F.,Lee, Matthew R.,Rose, Mark J.,Babij, Carol,Fernando, Manory,Hess, Kristen,Le, Quynh,Beltran, Pedro,Carnahan, Josette
, p. 6189 - 6192 (2009)
The discovery and optimization of a novel series of aminoisoquinolines as potent, selective, and efficacious inhibitors of the mutant B-Raf pathway is presented. The N-linked pyridylpyrimidine benzamide 2 was identified as a potent, modestly selective inhibitor of the B-Raf enzyme. Replacement of the benzamide with an aminoisoquinoline core significantly improved kinase selectivity and imparted favorable pharmacokinetic properties, leading to the identification of 1 as a potent antitumor agent in xenograft models. 2009 American Chemical Society.
