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Antiproliferative activity of ursolic acid/glycyrrhetinic acid-uracil/thymine hybrids

  • Li Sun
  • Xiang-Wu Chu
  • Chun-mei Liu
  • Li-Xin Sheng
  • Zhuan-Xin Chen
  • Ke-Guang ChengEmail author
Original Research
  • 12 Downloads

Abstract

As pharmacophore hybridization has been used frequently in the discovery of new drugs, ursolic acid/glycyrrhetinic acid-uracil/thymine hybrids have been synthesized and evaluated their antiproliferative activity by the MTT assay. The results displayed that, the hybrids of glycyrrhetinic acid (7a7b to 10a10b) exhibited slightly better antiproliferative activity than that of ursolic acid hybrids (3a3b to 6a6b). Two single glycyrrhetinic acid-thymine hybrids (8a and 10a) possessed good antiproliferative activity against tested A549 cell line (IC50 = 10.7 and 18.3 µM, respectively). And three hybrids (3a, 5a, and 10b) exhibited about 80% inhibitory ratio against tested Hela cell line.

Keywords

Ursolic acid Glycyrrhetinic acid Uracil Thymine Antiproliferative activity 

Notes

Acknowledgements

This study was financially supported by grants from the National Natural Science Foundation of PRC (21562006), Guangxi Natural Science Foundation of China (2015GXNSFAA139186), Guangxi′s Medicine Talented Persons Small Highland Foundation (1506), Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University), and Ministry of Educationof China (CMEMR2013-A01, CMEMR2013-C02).

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

44_2019_2344_MOESM1_ESM.doc (11.8 mb)
Supplementary Infoprmation

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Copyright information

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

Authors and Affiliations

  • Li Sun
    • 1
  • Xiang-Wu Chu
    • 1
  • Chun-mei Liu
    • 1
  • Li-Xin Sheng
    • 1
  • Zhuan-Xin Chen
    • 1
  • Ke-Guang Cheng
    • 1
    Email author
  1. 1.State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy of Guangxi Normal UniversityGuilinP. R. China

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