Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.

Abstract

A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme.

DOI: 10.1016/j.bmcl.2009.12.099