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

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

文献索引：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

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被引用次数: 48

摘要

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.