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Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase |
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| Authors: | Piatnitski Evgueni L Duncton Matthew A J Kiselyov Alexander S Katoch-Rouse Reeti Sherman Dan Milligan Daniel L Balagtas Chris Wong Wai C Kawakami Joel Doody Jacqueline F |
| Institution: | Department of Chemistry, ImClone Systems, 710 Parkside Avenue, Suite 2, Brooklyn, NY 11226, USA. |
| Abstract: | A novel class of 4-arylamino-phthalazin-1-yl-benzamides is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display potent VEGFR-2 inhibitory activity with an IC50 as low as 0.078 microM in an HTRF enzymatic assay. These compounds are relatively selective against a small kinase panel. |
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