Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372919 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,