Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents

Haijun Chen, Yu Gao, Ailan Wang, Xiaobin Zhou, Yunquan Zheng, Jia Zhou

Research output: Contribution to journalShort surveypeer-review

113 Scopus citations


Currently, there is a renewed interest in common dietaries and plant-based traditional medicines for the prevention and treatment of cancer. In the search for potential anticancer agents from natural sources, ursolic acid (UA), a pentacyclic triterpenoid widely found in various medicinal herbs and fruits, exhibits powerful biological effects including its attractive anticancer activity against various types of cancer cells. However, the limited solubility, rapid metabolism and poor bioavailability of UA restricted its further clinical applications. In the past decade, with substantial progress toward the development of new chemical entities for the treatment of cancer, numerous UA derivatives have been designed and prepared to overcome its disadvantages. Despite extensive effort, discovery of effective UA derivatives has so far met with only limited success. This review summarizes the current status of the structural diversity and evolution in medicinal chemistry of UA analogues and provides a detailed discussion of future direction for further research in the chemical modifications of UA.

Original languageEnglish (US)
Pages (from-to)648-655
Number of pages8
JournalEuropean journal of medicinal chemistry
StatePublished - Mar 6 2015


  • Anticancer agents
  • Chemical biology
  • Drug discovery
  • Natural products
  • Ursolic acid derivatives

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


Dive into the research topics of 'Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents'. Together they form a unique fingerprint.

Cite this