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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…

文献索引: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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被引用次数: 20

摘要

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.