Synthesis and cytotoxicity studies of novel benzhydrylpiperazine carboxamide and thioamide derivatives

J Enzyme Inhib Med Chem. 2014 Apr;29(2):205-14. doi: 10.3109/14756366.2013.765416. Epub 2013 Feb 8.

Abstract

Synthesis and cytotoxic activities of 32 benzhydrylpiperazine derivatives with carboxamide and thioamide moieties were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. In general, 4-chlorobenzhydrylpiperazine derivatives were more cytotoxic than other compounds. In addition, thioamide derivatives (6a-g) have higher growth inhibition than their carboxamide analogs.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Benzhydryl Compounds / chemical synthesis*
  • Benzhydryl Compounds / chemistry
  • Benzhydryl Compounds / pharmacology
  • Cell Culture Techniques
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Humans
  • Molecular Structure
  • Piperazines / chemical synthesis*
  • Piperazines / chemistry
  • Piperazines / pharmacology
  • Thioamides / chemical synthesis*
  • Thioamides / chemistry
  • Thioamides / pharmacology

Substances

  • Antineoplastic Agents
  • Benzhydryl Compounds
  • Piperazines
  • Thioamides