Medicinal Chemistry Research

, Volume 26, Issue 12, pp 3367–3374 | Cite as

Synthesis and biological evaluation of disulfides bearing 1,2,4-triazole moiety as antiproliferative agents

  • Xue-Feng Wang
  • Shuai Zhang
  • Bao-Lin Li
  • Ji-Jun Zhao
  • Yu-Ming Liu
  • Rui-Lian Zhang
  • Bo Li
  • Bao-Quan Chen
Original Research
  • 168 Downloads

Abstract

A series of novel nonsymmetrical disulfides bearing 1,2,4-triazole moiety were designed, synthesized, and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 8ar exhibited good antiproliferative activities, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 8l showed significant antiproliferative activity against SMMC-7721 cells with IC50 value of 2.97 μM. Compound 8f displayed highly effective biological activity against Hela cells with IC50 value of 3.51 μM. Compound 8d exhibited the best inhibitory effect against A549 cells with IC50 value of 2.79 μM. Furthermore, some of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.

Keywords

Disulfides 1,2,4-Triazole Antiproliferative activity 

Notes

Acknowledgements

We are grateful to the National Natural Science Foundation of China (20971097) and Tianjin Municipal Natural Science Foundation (13JCYBJC24500) for financial support.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no competing interests.

Supplementary material

44_2017_2029_MOESM1_ESM.doc (443 kb)
Supplementary Information

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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  • Xue-Feng Wang
    • 1
  • Shuai Zhang
    • 1
  • Bao-Lin Li
    • 1
  • Ji-Jun Zhao
    • 1
  • Yu-Ming Liu
    • 1
  • Rui-Lian Zhang
    • 1
  • Bo Li
    • 1
  • Bao-Quan Chen
    • 1
  1. 1.School of Chemistry and Chemical Engineering, Tianjin Key Laboratory of Organic Solar Cells and Photochemical ConversionTianjin University of TechnologyTianjinChina

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