Bioorganic & Medicinal Chemistry Letters 2006-03-15

Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.

Matthew A J Duncton, Evgueni L Piatnitski, Reeti Katoch-Rouse, Leon M Smith, Alexander S Kiselyov, Daniel L Milligan, Chris Balagtas, Wai C Wong, Joel Kawakami, Jacqueline F Doody

文献索引：Bioorg. Med. Chem. Lett. 16 , 1579, (2006)

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摘要

A novel class of 1-(isoquinolin-5-yl)-4-arylamino-phthalazines is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity with an IC(50) as low as 0.017 microM in an HTRF enzymatic assay. The compounds also inhibit VEGFR-1, a related tyrosine kinase.