Synthesis and biological activities of pyrazolo[3,4-g]quinoxaline derivatives

Eur J Med Chem. 2010 Nov;45(11):5520-6. doi: 10.1016/j.ejmech.2010.08.067. Epub 2010 Sep 15.

Abstract

The synthesis of new pyrazolo[3,4-g]quinoxaline derivatives, as well as their Pim kinases (Pim-1, Pim-2, Pim-3) inhibitory potencies and in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid cancer cell lines (PA1, PC3 and DU145) are described. The results obtained in this preliminary structure-activity relationship study have pointed out that most of the compounds in this series exhibited interesting in vitro Pim-3 kinase inhibitory potencies. Moreover, some of the tested compounds have demonstrated favorable antiproliferative potencies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Humans
  • Magnetic Resonance Spectroscopy
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology*
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization
  • Spectrophotometry, Infrared
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyrazoles
  • Quinoxalines