Synthesis and biological activities of dithiocarbamates containing 2(5H)-furanone-piperazine

Eur J Med Chem. 2018 Jul 15:155:165-170. doi: 10.1016/j.ejmech.2018.05.056. Epub 2018 Jun 4.

Abstract

A series of new dithiocarbamates containing a 2(5H)-furanone-piperazine group was synthesized. These compounds show good in vitro cytoxic activity. Among them, compound 6c exhibits the best inhibitory activity against HeLa cell lines with an IC50 of 0.06 ± 0.01 μM for 72 h, and it has good inhibitory activity against SMMC-7721 cell lines with an IC50 of 0.006 ± 0.04 μM for 72 h, but the toxicity was lower against LO2 cell lines with an IC50 of 45.76 ± 0.01 μM. The result showed that compound 6c is far more cytoxic towards cancer cell lines than towards benign cell lines compared with cytosine arabinoside (ARA) in vitro.

Keywords: 2(5H)-Furanone; Biological activities; Dithiocarbamates; SMMC-7721 cell lines; Synthesis.

MeSH terms

  • Apoptosis / drug effects
  • Cell Line
  • Dose-Response Relationship, Drug
  • Furans / chemistry
  • Furans / pharmacology*
  • Humans
  • Molecular Structure
  • Piperazines / chemistry
  • Piperazines / pharmacology*
  • Structure-Activity Relationship
  • Thiocarbamates / chemical synthesis
  • Thiocarbamates / chemistry
  • Thiocarbamates / pharmacology*

Substances

  • Furans
  • Piperazines
  • Thiocarbamates