An Update on the Recent Advances and Discovery of Novel Tubulin Colchicine Binding Inhibitors

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.

Graphical Abstract

Keywords: :

• antiproliferative effect
• colchicine binding site
• SARs
• structure modification
• tubulin polymerization inhibitors

Financial & competing interests disclosure

This work was supported by the grant from the National Natural Science Foundation of China (no. 82173679). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.