咪唑类和苯并咪唑作为微管蛋白-调节剂治疗癌症

Title:Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy

Volume: 22 Issue: 11

Author(s): Fernando C. Torres, M. Eugenia Garcia-Rubino, Cesar Lozano-Lopez, Daniel F. Kawano, Vera L. Eifler-Lima and Gilsane L. von Poser and Joaquin M. Campos

Affiliation:

关键词: 抗癌，苯并咪唑，秋水仙碱结合位点，咪唑，老药新用，微管蛋白

摘要: 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.

Cite this article as:

Fernando C. Torres, M. Eugenia Garcia-Rubino, Cesar Lozano-Lopez, Daniel F. Kawano, Vera L. Eifler-Lima and Gilsane L. von Poser and Joaquin M. Campos , Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy, Current Medicinal Chemistry 2015; 22 (11) . https://dx.doi.org/10.2174/0929867322666150114164032