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

Abstract

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.

Citation

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. https://doi.org/10.4155/fmc-2022-0212

• 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 Ltd
• Peer Reviewed: Peer Reviewed
• Volume: 15
• Issue: 1
• Pages: 73-95
• DOI: https://doi.org/10.4155/fmc-2022-0212
• Keywords: Aantiproliferative effect; colchicine binding site; SARs; structure modification; tubulin polymerization inhibitors
• Public URL: https://nottingham-repository.worktribe.com/output/17197217
• Publisher URL: https://www.future-science.com/doi/10.4155/fmc-2022-0212