| Literature DB >> 19101155 |
Matthew A J Duncton1, Eugene L Piatnitski Chekler, Reeti Katoch-Rouse, Dan Sherman, Wai C Wong, Leon M Smith, Joel K Kawakami, Alexander S Kiselyov, Daniel L Milligan, Chris Balagtas, Yaron R Hadari, Ying Wang, Sheetal N Patel, Robin L Rolster, James R Tonra, David Surguladze, Stan Mitelman, Paul Kussie, Peter Bohlen, Jacqueline F Doody.
Abstract
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 exposure when dosed orally to female CD-1 mice.Entities:
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Year: 2008 PMID： 19101155 DOI： 10.1016/j.bmc.2008.11.049
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641