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An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors

Weng, Haoxiang; Li, Jinlong; Zhu, Huajian; Carver Wong, Kei Fung; Zhu, Zheying; Xu, Jinyi


Haoxiang Weng

Jinlong Li

Huajian Zhu

Kei Fung Carver Wong

Associate Professor in International Pharmacy and Traditional Medicines

Jinyi Xu


Microtubules, formed by α- and β-tubulin heterodimer, are considered as a major target to prevent the proliferation of tumor cells. Microtubule-targeted agents have become increasingly effective anticancer drugs. However, due to the relatively sophisticated chemical structure of taxane and vinblastine, their application has faced numerous obstacles. Conversely, the structure of colchicine binding site inhibitors (CBSIs) is much easier to be modified. Moreover, CBSIs have strong antiproliferative effect on multidrug-resistant tumor cells and have become the mainstream research orientation of microtubule-targeted agents. This review focuses mainly on the recent advances of CBSIs during 2017–2022, attempts to depict their biological activities to analyze the structure–activity relationships and offers new perspectives for designing next generation of novel CBSIs.


Weng, H., Li, J., Zhu, H., Carver Wong, K. F., Zhu, Z., & Xu, J. (2023). An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors. Future Medicinal Chemistry, 15(1), 73-95.

Journal Article Type Review
Acceptance Date Jan 18, 2023
Online Publication Date Feb 9, 2023
Publication Date 2023-01
Deposit Date Feb 11, 2023
Publicly Available Date Feb 1, 2024
Journal Future Medicinal Chemistry
Print ISSN 1756-8919
Electronic ISSN 1756-8927
Publisher Future Science
Peer Reviewed Peer Reviewed
Volume 15
Issue 1
Pages 73-95
Keywords Aantiproliferative effect; colchicine binding site; SARs; structure modification; tubulin polymerization inhibitors
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