Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors

A novel series of potent heteroaryl-ketone derivatives active against VEGFR-2 kinase is described. The best compounds were demonstrated to be inactive against a panel of tyrosine and serine/threonine kinases with the exception of VEGFR-1 kinase. Selected representatives displayed acceptable exposure levels when administered orally to mice.