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

Microtubules, formed by alpha- and beta-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.

Automated summary

Microtubules are a major target for inhibiting tumor cell proliferation, and microtubule-targeted agents have become increasingly effective in cancer treatment. Colchicine binding site inhibitors (CBSIs) have a simpler chemical structure than taxane and vinblastine, making them easier to modify. Furthermore, CBSIs have a strong antiproliferative effect on multidrug-resistant tumor cells and have become the mainstream research focus in the development of microtubule-targeted agents.