Arylphthalazines: Identification of a new phthalazine chemotype as inhibitors of VEGFR kinase

…, MAJ Duncton, AS Kiselyov, R Katoch-Rouse…

Index: Piatnitski, Evgueni L.; Duncton, Matthew A. J.; Kiselyov, Alexander S.; Katoch-Rouse, Reeti; Sherman, Dan; Milligan, Daniel L.; Balagtas, Chris; Wong, Wai C.; Kawakami, Joel; Doody, Jacqueline F. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4696 - 4698

Full Text: HTML

Citation Number: 48

Abstract

A novel class of 4-arylamino-phthalazin-1-yl-benzamides is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display potent VEGFR-2 inhibitory activity with an IC50 as low as 0.078 μM in an HTRF enzymatic assay. These compounds are relatively selective against a small kinase panel.