title: Imidazoles and benzimidazoles as tubulin-modulators for anti-cancer therapy.
abstract: 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.
authors.forename: Fernando C
authors.initials: FC
authors.lastname: Torres
authors.forename: M Eugenia
authors.initials: ME
authors.lastname: García-Rubiño
authors.forename: César
authors.initials: C
authors.lastname: Lozano-López
authors.forename: Daniel F
authors.initials: DF
authors.lastname: Kawano
authors.forename: Vera L
authors.initials: VL
authors.lastname: Eifler-Lima
authors.forename: Gilsane L
authors.initials: GL
authors.lastname: von Poser
authors.affiliation: Departamento de Quimica Farmaceutica y Organica, Facultad de Farmacia, Campus de Cartuja s/n, 18071 Granada, Spain. jmcampos@ugr.es.
authors.forename: Joaquín M
authors.initials: JM
authors.lastname: Campos
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D014404:Tubulin / Q000378:metabolism*; D050257:Tubulin Modulators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D007093:Imidazoles; D014404:Tubulin; D050257:Tubulin Modulators