Discovery and development of natural product oridonin-inspired anticancer agents

Ye Ding, Chunyong Ding, Na Ye, Zhiqing Liu, Eric A. Wold, Haiying Chen, Christopher Wild, Qiang Shen, Jia Zhou

Research output: Contribution to journalReview articlepeer-review

87 Scopus citations


Natural products have historically been, and continue to be, an invaluable source for the discovery of various therapeutic agents. Oridonin, a natural diterpenoid widely applied in traditional Chinese medicines, exhibits a broad range of biological effects including anticancer and anti-inflammatory activities. To further improve its potency, aqueous solubility and bioavailability, the oridonin template serves as an exciting platform for drug discovery to yield better candidates with unique targets and enhanced drug properties. A number of oridonin derivatives (e.g. HAO472) have been designed and synthesized, and have contributed to substantial progress in the identification of new agents and relevant molecular mechanistic studies toward the treatment of human cancers and other diseases. This review summarizes the recent advances in medicinal chemistry on the explorations of novel oridonin analogues as potential anticancer therapeutics, and provides a detailed discussion of future directions for the development and progression of this class of molecules into the clinic.

Original languageEnglish (US)
Pages (from-to)102-117
Number of pages16
JournalEuropean journal of medicinal chemistry
StatePublished - 2016


  • Anticancer agents
  • Chemical biology
  • Diterpenoids
  • Drug discovery
  • Natural product
  • Oridonin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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