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

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

Bioorganic & medicinal chemistry letters (2011-06-03)
Craig A Zificsak, Jay P Theroff, Lisa D Aimone, Thelma S Angeles, Mark S Albom, Mangeng Cheng, Eugen F Mesaros, Gregory R Ott, Matthew R Quail, Ted L Underiner, Weihua Wan, Bruce D Dorsey
PMID21632243
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.