Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.

ID: ALA1795227

Journal: Bioorg Med Chem Lett

Title: Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.

Authors: Zificsak CA, Theroff JP, Aimone LD, Angeles TS, Albom MS, Cheng M, Mesaros EF, Ott GR, Quail MR, Underiner TL, Wan W, Dorsey BD.

Abstract: The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was achieved by conversion of the 2-amino group into a methanesulfonamide. Tumor growth inhibition was observed when an orally bioavailable analog was evaluated in a Karpas-299 tumor xenograft mouse model.

CiteXplore: 21632243

DOI: 10.1016/j.bmcl.2011.05.040

Patent ID: ┄