Pyrazoline bearing benzimidazoles: search for anticancer agent

Eur J Med Chem. 2010 Jan;45(1):114-9. doi: 10.1016/j.ejmech.2009.09.032. Epub 2009 Sep 23.

Abstract

2-acetyl benzimidazole was allowed to react with substituted aromatic aldehydes to get desired intermediate chalcones (2a-g), the cyclocondensation of these intermediates with hydrazine hydrate and phenyl hydrazine in two separate reactions yielded pyrazoline derivatives (3a-g &4a-g respectively). Among the synthesize compounds, six compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10(-5) M) in full NCI 60 cell panel. Among the selected compounds, (4f) 2-[5-(3,4-dimethoxyphenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1H-benzimidazole (NSC 748326) was found to be the most active candidate of the series and selected for further evaluation at five dose level screening.

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology*
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Drug Discovery*
  • Humans
  • Pyrazoles / chemistry*

Substances

  • Antineoplastic Agents
  • Benzimidazoles
  • Pyrazoles
  • pyrazole
  • benzimidazole