2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents

Bioorg Med Chem Lett. 2019 Mar 15;29(6):806-810. doi: 10.1016/j.bmcl.2019.01.025. Epub 2019 Jan 23.

Abstract

A series of novel 2-benzoylbenzofuran derivatives possessing piperazine linker have been prepared, and their in vitro anticancer activity against a panel of human tumor cell lines by MTT assay were evaluated. The results demonstrated that tertiary amine derivatives exhibited better cytotoxic activity, and SAR study revealed that electron-donating substituents on the phenyl ring of the derivatization functionality contributed to potent anticancer activities. Among them, compounds 6, 9, 11, 18, 23 and 25 displayed both better anti-tumor activity and lower cytotoxic effect on human normal liver cell L02. Further apoptosis analysis showed that compound 18 significantly induced apoptosis in A549 cell, which was considered as the most potent anticancer agent.

Keywords: 2-Benzoylbenzofuran; Anticancer activity; Apoptosis; Cytotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Apoptosis / drug effects
  • Benzofurans / chemical synthesis
  • Benzofurans / pharmacology*
  • Benzofurans / toxicity
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Piperazines / chemical synthesis
  • Piperazines / pharmacology*
  • Piperazines / toxicity
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Benzofurans
  • Piperazines