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Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II |
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| Authors: | 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 |
| Institution: | Department of Chemistry, ImClone Systems, 710 Parkside Avenue, Suite 2, Brooklyn, NY 11226, USA. mattduncton@yahoo.com |
| Abstract: | 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. |
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