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

Zificsak, Craig A; Theroff, Jay P; Aimone, Lisa D; Angeles, Thelma S; Albom, Mark S; Cheng, Mangeng; Mesaros, Eugen F; Ott, Gregory R; Quail, Matthew R; Underiner, Ted L; Wan, Weihua; Dorsey, Bruce D.
Bioorg Med Chem Lett; 21(13): 3877-80, 2011 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-21632243
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.
Selo DaSilva