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Medicinal Chemistry Research

, Volume 28, Issue 10, pp 1718–1725 | Cite as

Synthesis and antitumor evaluation of novel fused heterocyclic 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives

  • Xiao-Jia Liu
  • Hai-Ying Liu
  • Hai-Xin Wang
  • Yan-Ping ShiEmail author
  • Rui Tang
  • Shuai Zhang
  • Bao-Quan ChenEmail author
Original Research
  • 51 Downloads

Abstract

In this study, twenty three 3,6-disubstituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives were synthesized and their antiproliferative activities in vitro were studied against SMMC-7721, HeLa, A549, and L929 by the CCK-8 assay. The bioassay results demonstrated that all tested compounds 8(aw) exhibited antiproliferation with different degrees, and some compounds showed better effects than reference drug 5-fluorouracil. Among these screened compounds, compounds 8a, 8d, and 8l displayed significant antitumor activities in inhibiting SMMC-7721cell proliferation with IC50 values of 1.64, 1.74, and 1.61 µM, respectively. Compounds 8d and 8l were manifested highly effective biological activity versus HeLa cells with IC50 values of 2.23 and 2.84 µM, respectively. Compound 8l was found to have the highest antitumor potency against A549 cells with IC50 value of 2.67 µM. Furthermore, all compounds exhibited weaker cytotoxic effects than 5-fluorouracil on normal cell lines L929.

Keywords

Triazolo-thiadiazole Disulfides Antitumor activity 

Notes

Acknowledgements

We are grateful to the Tianjin Municipal Natural Science Foundation (18JCYBJC94900) and Training Project of Innovation Team of Colleges and Universities in Tianjin (TD13-5020) for financial support.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

44_2019_2409_MOESM1_ESM.docx (3.2 mb)
Supplementary Material

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  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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