- 2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
Bioorganic & medicinal chemistry letters (2003-05-06)
Peter J Manley, Adrienne E Balitza, Mark T Bilodeau, Kathleen E Coll, George D Hartman, Rosemary C McFall, Keith W Rickert, Leonard D Rodman, Kenneth A Thomas
PMID12729639
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).
MATERIALS