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

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3136-40. doi: 10.1016/j.bmcl.2007.03.031. Epub 2007 Mar 15.

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.

MeSH terms

  • Animals
  • Humans
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology*
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*

Substances

  • Protein Kinase Inhibitors
  • Pyrazoles
  • Receptor Protein-Tyrosine Kinases