Design, synthesis and anticancer activity of novel hybrid compounds between benzofuran and N-aryl piperazine

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3421-4. doi: 10.1016/j.bmcl.2016.06.055. Epub 2016 Jun 21.

Abstract

A series of novel hybrid compounds between benzofuran and N-aryl piperazine have been designed and prepared. These derivatives were evaluated for their in vitro anti-tumor activity against a panel of human tumor cell lines by MTT assay. The results demonstrated that amide derivatives were more bioactive than sulfonamide compounds in general, and that chloro or trifluoromethyl substituent was vital for modulating cytotoxic activity. In particular, compound 13 was found to be the most potent compound against 4 strains human tumor cell lines, and exhibited cytotoxic activity selectively against Hela (0.03μM).

Keywords: Anticancer activity; Benzofuran; Hybrid compounds; N-Aryl piperazine.

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Benzofurans / chemistry
  • Benzofurans / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Piperazine
  • Piperazines / chemistry
  • Piperazines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Benzofurans
  • Piperazines
  • Piperazine
  • benzofuran