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ID: ALA1136377

Journal: Bioorg Med Chem Lett

Title: 2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.

Authors: Manley PJ, Balitza AE, Bilodeau MT, Coll KE, Hartman GD, McFall RC, Rickert KW, Rodman LD, Thomas KA.

Abstract: 2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound 1 (KDR IC(50)=105 nM, Cell IC(50)=8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative 2d (KDR IC(50)=6 nM, cell IC(50)=19 nM).

CiteXplore: 12729639

DOI: 10.1016/s0960-894x(03)00244-0