Imidazoles and benzimidazoles are privileged heterocyclic bioactive compounds used with
success in the clinical practice of innumerous diseases. Although there are many advancements in cancer
therapy, microtubules remain as one of the few macromolecular targets validated for planning active
anti-cancer compounds, and the design of drugs that modulate microtubule dynamics in unknown
sites of tubulin is one of the goals of the medicinal chemistry. The discussion of the role of new and
commercially available imidazole and benzimidazole derivatives as tubulin modulators is scattered
throughout scientific literature, and indicates that these compounds have a tubulin modulation mechanism different from
that of tubulin modulators clinically available, such as paclitaxel, docetaxel, vincristine and vinblastine. In fact, recent literature
indicates that these derivatives inhibit microtubule formation binding to the colchicine site, present good pharmacokinetic
properties and are capable of overcoming multidrug resistance in many cell lines. The understanding of the
mechanisms involved in the imidazoles/benzimidazoles modulation of microtubule dynamics is very important to develop
new strategies to overcome the resistance to anti-cancer drugs and to discover new biomarkers and targets for cancer chemotherapy.
Keywords: Anti-tumour, benzimidazole, colchicine-binding site, imidazole, reposition of old drugs, tubulin.
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