The use of naphthoquinones and furano-naphthoquinones as anti-invasive agents

Nga Yi Tsang, Wai I. Chik, Lai Pan Sze, Ming Zhong Wang, Siu Wai Tsang, Hongjie Zhang*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

10 Citations (Scopus)


Background: Cancer is a leading cause of mortality in the world and metastasis is to blame. A number of naphthoquinones (NQs) have shown ability to reduce cancer stemness and metastatic potential. Furano-naphthoquinones (FNQs), which is a class of NQ characterized by the incorporation of an additional furan ring, have demonstrated improved anti-cancer potency as compared to the other classes of NQs. Objective: In this study, the natural origins, synthetic routes and derivatives of migrastatic NQs were reviewed. The anti-invasive and anti-metastatic mechanisms of NQs and the more powerful FNQs in targeting cancer were also discussed. Method: The articles related to the anti-invasive mechanisms of NQs were comprehensively reviewed. The plant origins, synthetic routes and antitumor effects of more than 360 FNQs were also covered and presented according to their chemical structures. Results: Anti-cancer NQs inhibit cancer invasion by acting on epithelial–mesenchymal transition (EMT), cancer stem cells (CSCs) and signal transducer and activator of transcription 3 (STAT3) signaling. BBI608, a natural FNQ, has entered phases I and II clinical trials. It has been regarded as a potential candidate for new-generation lead compound acting directly on CSCs to overcome the problem of chemotherapy resistance. Apart from the plant-derived FNQs, there are a number of synthetic FNQs that were found to intervene in cancer invasion and metastasis. Conclusion: The anti-invasive mechanisms of NQs have been thoroughly studied. FNQs generally show higher anti-cancer activity than that of NQs. The mechanisms of action of FNQs are worth further investigation.

Original languageEnglish
Pages (from-to)5007-5056
Number of pages50
JournalCurrent Medicinal Chemistry
Issue number38
Publication statusPublished - Nov 2018

Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • Anti-cancer
  • Anti-invasive
  • BBI608
  • Cancer stemness
  • Chemical synthesis
  • CSC
  • EMT
  • Furanonaphthoquinone
  • Naphthoquinone
  • Natural products
  • STAT3


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