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).
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