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

doi:10.1016/j.bmc.2008.11.049

Residential College	false
Status	已發表Published
	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 Publication	Bioorganic and Medicinal Chemistry
ISSN	09680896
Volume	17 Issue:2 Pages:731-740
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. © 2008 Elsevier Ltd. All rights reserved.
Keyword	Angiogenesis Arylphthalazine Inhibitor Kdr Kinase Phthalazine Vegfr-2
DOI	10.1016/j.bmc.2008.11.049
URL	View the original
Language	英語English
WOS ID	WOS:000262708300036
Scopus ID	2-s2.0-58549103895
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics
Document Type	Journal article
Collection	University of Macau
Affiliation	Eli 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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