Synthesis and in vitro antiproliferative evaluation of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4414-4416. doi: 10.1016/j.bmcl.2016.08.014. Epub 2016 Aug 6.

Abstract

A series of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against SMMC-7721, Hela and A549 human cancer cell lines by CCK-8 assay. The preliminary bioassay results demonstrated that all tested compounds 7a-7o exhibited antiproliferation with different degrees, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 7j showed significant antiproliferative activity against SMMC-7721 cells with IC50 value of 3.40μM. Compound 7a displayed highly effective biological activity against Hela cells with IC50 value of 4.26μM. Compound 7g exhibited the best inhibitory effect against A549 cells with IC50 value of 6.26μM.

Keywords: 1,3,4-Oxadiazole; Antiproliferative activity; Nonsymmetrical disulfides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Disulfides / chemistry*
  • Fluorouracil / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Oxadiazoles / chemistry*

Substances

  • Antineoplastic Agents
  • Disulfides
  • Oxadiazoles
  • 1,3,4-oxadiazole
  • Fluorouracil