1-Oxo-3-aryl-1H-indene-2-carboxylic acid derivatives as selective inhibitors of fibroblast growth factor receptor-1 tyrosine kinase

…, GH Lu, AJ Kraker, A Amar, B Hartl, JM Hamby…

文献索引：Barvian; Panek; Lu; Kraker; Amar; Hartl; Hamby; Showalter Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 22 p. 2903 - 2908

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被引用次数: 11

摘要

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 ...