Design and synthesis of oridonin derivatives as cytotoxic agents

Chen Liang Zhao, Chi Yuan Zhang, Xiao Min Yang, Ka Hei Lam, Yi Xuan Xia, Yin Xiao Du, Lu Tai Pan, Hong Jie Zhang*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review


Oridonin is one of the ent-kaurane diterpenes that have been studied extensively for various bioactivities. In an effort to expand natural scaffold-based library as anticancer agents, we have designed and synthesised a number of novel oridonin derivatives and evaluated their bioactivities on a panel of human cancer cell lines (HCT116, A375, MCF-7, HepG2, and A549). Compound 4b bearing a 4-fluorophenyl moiety was found to be the most active compound with an IC50 value of 0.3 μM against MCF-7 cells, which was 7.4-fold more active than oridonin. This study could provide some insightful information for further synthesis of oridonin derivatives as anticancer agents.

Original languageEnglish
JournalNatural Product Research
Publication statusE-pub ahead of print - 30 Oct 2023

Scopus Subject Areas

  • Analytical Chemistry
  • Biochemistry
  • Plant Science
  • Organic Chemistry

User-Defined Keywords

  • anticancer
  • cytotoxicity
  • derivatives
  • ent-kaurane diterpenoid
  • Oridonin


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