Author/Authors :
M. R. Barvian، نويسنده , , R. L. Panek، نويسنده , , G. H. Lu، نويسنده , , A. J. Kraker، نويسنده , , A. Amar and A. J. Weiss، نويسنده , , B. Hartl، نويسنده , , J. M. Hamby، نويسنده , , H. D. H. Showalter، نويسنده ,
Abstract :
Fibroblast growth factor receptor (FGFr) mediated signal transduction is implicated in vascular proliferative diseases and some cancers. We have identified methyl 1-oxo-3-phenyl-1H-indene-2-carboxylic ester as a small molecule inhibitor of the tyrosine kinase activity of FGFr-1, (IC50 = 5.1 μM). We report here the synthesis and structure-activity studies about this template core. Additionally, screening of this series against a panel of tyrosine kinases shows selective inhibition of FGFr.
