Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors

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Abstract

A series of 1,4-dihydroindeno[1,2-c]pyrazoles was prepared and evaluated for their enzymatic inhibition of KDR kinase. Computer modeling studies revealed the importance of attaching a basic side chain in predicting the binding mode of those compounds. Further investigation of structure-activity relationships led to 19, a lead compound with an acceptable selectivity profile, activity in whole cells, and good oral efficacy in an estradiol-induced murine uterine edema model of VEGF activity. © 2006 Elsevier Ltd. All rights reserved.

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Dinges, J., Akritopoulou-Zanze, I., Arnold, L. D., Barlozzari, T., Bousquet, P. F., Cunha, G. A., … Zhang, H. Q. (2006). Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(16), 4371–4375. https://doi.org/10.1016/j.bmcl.2006.05.052

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