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Medicinal Chemistry Research

, Volume 28, Issue 2, pp 203–214 | Cite as

Design, synthesis, antiproliferative and antibacterial evaluation of quinazolinone derivatives

  • Hai-Xin Wang
  • Hai-Ying Liu
  • Wei Li
  • Shuai Zhang
  • Zheng Wu
  • Xin Li
  • Cai-Wen LiEmail author
  • Yu-Ming Liu
  • Bao-Quan ChenEmail author
Original Research
  • 45 Downloads

Abstract

A series of novel quinazolinone derivatives bearing a disulfide bond were designed and synthesized. Their in vitro antiproliferative activities were evaluated using CCK-8 assay against SMMC-7721, Hela, A549 and MCF-7 human cancer cell lines and normal cell lines L929. The preliminary bioassay results demonstrated that all compounds 7a7h, 8a8h and 9a9h exhibited antiproliferation with various degrees, and some compounds showed better effects than positive control 5-fluorouracil against different cancer cell lines. Among these compounds, 8c and 9f showed significant antiproliferative activity against SMMC-7721 cells with IC50 values of 2.88 and 2.56 μM, respectively. In Hela cells, compounds 9c and 9d showed highly effective biological activity with IC50 values of 3.16 and 2.68 μM, respectively. Compounds 7a and 9a exhibited good inhibitory effect against A549 cells with IC50 values of 3.53 and 3.54 μM, respectively. In MCF-7 cells, compounds 7e, 8e and 9e displayed excellent activity with IC50 values of 1.26, 1.12 and 1.85 μM, respectively. Besides, most of the tested compounds showed low cytotoxic effect against the normal cell lines L929. Biological evaluation indicated that all the tested compounds possessed antibacterial activity with certain degrees.

Keywords

Quinazolinone Disulfides Antiproliferative and antibacterial activities 

Notes

Acknowledgements

We are grateful to the National Natural Science Foundation of China (20971097), the Tianjin Municipal Natural Science Foundation (13JCYBJC24500) and the 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_2018_2276_MOESM1_ESM.pdf (2.9 mb)
Supplementary Information

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Copyright information

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

Authors and Affiliations

  • Hai-Xin Wang
    • 1
  • Hai-Ying Liu
    • 1
  • Wei Li
    • 1
  • Shuai Zhang
    • 1
  • Zheng Wu
    • 1
  • Xin Li
    • 1
  • Cai-Wen Li
    • 1
    Email author
  • Yu-Ming Liu
    • 1
  • Bao-Quan Chen
    • 1
    Email author
  1. 1.Tianjin Key Laboratory of Organic Solar Cells and Photochemical Conversion, School of Chemistry and Chemical EngineeringTianjin University of TechnologyTianjinChina

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