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Piatnitski, E.L. et al.

Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.

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.[1]

References

Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase. Piatnitski, E.L., Duncton, M.A., Kiselyov, A.S., Katoch-Rouse, R., Sherman, D., Milligan, D.L., Balagtas, C., Wong, W.C., Kawakami, J., Doody, J.F. Bioorg. Med. Chem. Lett. (2005) [Pubmed]

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