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

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.
Ji-Jun Zhao 1,  Xue-Feng Wang 1,  Bao-Lin Li 1,  Rui-Lian Zhang 1,  Bo Li 1,  Yu-Ming Liu 1,  Cai-Wen Li 1,  Jin-Biao Liu 1,  Bao-Quan Chen 2
Affiliations

Affiliations

  • 1 Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China.
  • 2 Department of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, PR China. Electronic address: chenbaoquan66@126.com.
PMID: 27542307 DOI: 10.1016/j.bmcl.2016.08.014
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.

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