Synthesis and biological evaluation of 5-substituted 1, 4-dihydroindeno [1, 2-c] pyrazoles as multitargeted receptor tyrosine kinase inhibitors

I Akritopoulou-Zanze, DH Albert, PF Bousquet…

Index: Akritopoulou-Zanze, Irini; Albert, Daniel H.; Bousquet, Peter F.; Cunha, George A.; Harris, Christopher M.; Moskey, Maria; Dinges, Jurgen; Stewart, Kent D.; Sowin, Thomas J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 11 p. 3136 - 3140

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Citation Number: 20

Abstract

We report the synthesis and biological evaluation of 5-substituted 1, 4-dihydroindeno [1, 2-c] pyrazoles as multitargeted kinase inhibitors. Initial efforts focused on the development of selective KDR inhibitors, while later strategies involved the improvement of potency toward multiple kinase targets. Thus, several compounds were identified as potent KDR, Flt1, Flt3, and c-Kit inhibitors.