Article
Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.
Journal of medicinal chemistry - 22 Oct 2009
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
Abstract excerpt
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...
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