Author/Authors :
Matthew A.J. Duncton، نويسنده , , Evgueni L. Piatnitski، نويسنده , , Reeti Katoch-Rouse، نويسنده , , Leon M. Smith II، نويسنده , , Alexander S. Kiselyov، نويسنده , , Daniel L. Milligan، نويسنده , , Chris Balagtas، نويسنده , , Wai C. Wong، نويسنده , , Joel Kawakami، نويسنده , , Jacqueline F. Doody، نويسنده ,
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 IC50 as low as 0.017 μM in an HTRF enzymatic assay. The compounds also inhibit VEGFR-1, a related tyrosine kinase.
Keywords :
Vascular endothelial growth factor , kinase inhibitor , angiogenesis , Phthalazine
