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Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2
Duncton M.A.J.; Piatnitski Chekler E.L.; Katoch-Rouse R.; Sherman D.; Wong W.C.; Smith II L.M.; Kawakami J.K.; Kiselyov A.S.; Milligan D.L.; Balagtas C.; Hadari Y.R.; Wang Y.; Patel S.N.; Rolster R.L.; Tonra J.R.; Surguladze D.; Mitelman S.; Kussie P.; Bohlen P.; Doody J.F.
2009-01-15
Source PublicationBioorganic and Medicinal Chemistry
ISSN09680896
Volume17Issue:2Pages:731-740
AbstractA 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. © 2008 Elsevier Ltd. All rights reserved.
KeywordAngiogenesis Arylphthalazine Inhibitor KDR Kinase Phthalazine VEGFR-2
DOI10.1016/j.bmc.2008.11.049
URLView the original
Language英語English
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Cited Times [WOS]:36   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
AffiliationEli Lilly and Company
Recommended Citation
GB/T 7714
Duncton M.A.J.,Piatnitski Chekler E.L.,Katoch-Rouse R.,et al. Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2[J]. Bioorganic and Medicinal Chemistry,2009,17(2):731-740.
APA Duncton M.A.J.,Piatnitski Chekler E.L.,Katoch-Rouse R.,Sherman D.,Wong W.C.,Smith II L.M.,Kawakami J.K.,Kiselyov A.S.,Milligan D.L.,Balagtas C.,Hadari Y.R.,Wang Y.,Patel S.N.,Rolster R.L.,Tonra J.R.,Surguladze D.,Mitelman S.,Kussie P.,Bohlen P.,&Doody J.F..(2009).Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2.Bioorganic and Medicinal Chemistry,17(2),731-740.
MLA Duncton M.A.J.,et al."Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2".Bioorganic and Medicinal Chemistry 17.2(2009):731-740.
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