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.
Meng-Xue Wei  1 ,  Jiao Zhang  2 ,  Fu-Li Ma  2 ,  Ming Li  2 ,  Jia-Ying Yu  2 ,  Wei Luo  2 ,  Xue-Qiang Li  3
Affiliations
  • 1. State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan, 750021, China. Electronic address: [email protected].
  • 2. State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan, 750021, China.
  • 3. State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan, 750021, China. Electronic address: [email protected].
PMID: 29886320 DOI: 10.1016/j.ejmech.2018.05.056
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.