Duncton Matthew A J, Piatnitski Evgueni L, Katoch-Rouse Reeti, Smith Leon M, Kiselyov Alexander S, Milligan Daniel L, Balagtas Chris, Wong Wai C, Kawakami Joel, Doody Jacqueline F
Department of Chemistry, ImClone Systems, 710 Parkside Avenue, Suite 2, Brooklyn, NY 11226, USA.
Bioorg Med Chem Lett. 2006 Mar 15;16(6):1579-81. doi: 10.1016/j.bmcl.2005.12.045. Epub 2005 Dec 28.
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.
一类新型的1-(异喹啉-5-基)-4-芳基氨基酞嗪被描述为血管内皮生长因子受体II（VEGFR-2）的抑制剂。在HTRF酶促试验中，许多化合物表现出VEGFR-2抑制活性，IC(50)低至0.017微摩尔。这些化合物还抑制相关的酪氨酸激酶VEGFR-1。
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