Potent 2-[(Pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based Inhibitors of VEGFR-2 (KDR) Kinase

Pyrimidino-thiazolyl carbonitriles were prepared that are potent VEGFR-2 (KDR) kinase inhibitors. The modification of lead structures resulted in 3m which exhibited the best overall profile in KDR inhibitory activity, iv/po pharmacokinetics, and reduced hERG affinity.