1-OXO-3-ARYL-1H-INDENE-2-CARBOXYLIC ACID-DERIVATIVES AS SELECTIVE INHIBITORS OF FIBROBLAST GROWTH-FACTOR RECEPTOR-1 TYROSINE KINASE

Authors
BARVIAN MR PANEK RL LU GH KRAKER AJ AMAR A HARTL B HAMBY JM SHOWALTER HDH
Citation
Mr. Barvian et al., 1-OXO-3-ARYL-1H-INDENE-2-CARBOXYLIC ACID-DERIVATIVES AS SELECTIVE INHIBITORS OF FIBROBLAST GROWTH-FACTOR RECEPTOR-1 TYROSINE KINASE, Bioorganic & medicinal chemistry letters, 7(22), 1997, pp. 2903-2908
Citations number
19
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
22
Year of publication
1997
Pages
2903 - 2908
Database
ISI
SICI code
0960-894X(1997)7:22<2903:1AASI>2.0.ZU;2-X
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 mu M). We report here the synthesis and structure-activity studies about this template core. Additionally, screening of this ser ies against a panel of tyrosine kinases shows selective inhibition of FGFr. (C) 1997 Elsevier Science Ltd.