Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2

MAJ Duncton, ELP Chekler, R Katoch-Rouse…

文献索引：Duncton, Matthew A.J.; Piatnitski Chekler, Eugene L.; Katoch-Rouse, Reeti; Sherman, Dan; Wong, Wai C.; Smith II, Leon M.; Kawakami, Joel K.; Kiselyov, Alexander S.; Milligan, Daniel L.; Balagtas, Chris; Hadari, Yaron R.; Wang, Ying; Patel, Sheetal N.; Rolster, Robin L.; Tonra, James R.; Surguladze, David; Mitelman, Stan; Kussie, Paul; Bohlen, Peter; Doody, Jacqueline F. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 2 p. 731 - 740

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被引用次数: 23

摘要

A series of arylphthalazine derivatives were synthesized and evaluated as antagonists of VEGF receptor II (VEGFR-2). IM-094482 57, which was prepared in two steps from commercially available starting materials, was found to be a potent inhibitor of VEGFR-2 in enzymatic, cellular and mitogenic assays (comparable activity to ZD-6474). Additionally, 57 inhibited the related receptor, VEGF receptor I (VEGFR-1), and showed excellent ...