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

  • Dinges J
  • Akritopoulou-Zanze I
  • Arnold L
 et al. 
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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.

Author-supplied keywords

  • 1,4-Dihydroindeno[1,2-c]pyrazoles
  • Cancer
  • Inhibitor
  • KDR kinase
  • Receptor tyrosine kinase

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  • Jürgen Dinges

  • Irini Akritopoulou-Zanze

  • Lee D. Arnold

  • Teresa Barlozzari

  • Peter F. Bousquet

  • George A. Cunha

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