摘要
咪唑类和苯并咪唑是特有的杂环生物活性化合物,已成功用于众多疾病的临床治疗。虽然癌症治疗领域有很多的研究进展,但微管成为为数不多的已验证活性抗癌物质的大分子靶标,设计调节微管动力学在微管蛋白的未知结合位点是药物化学的目标之一。讨论新型商用咪唑和苯并咪唑衍生物作为微管蛋白调节器在很多科学文献都有提到,并表明这些化合物的微管蛋白调制机制不同于临床上现有的微管蛋白调节器,如紫杉醇、多西紫杉醇、长春新碱和长春花碱。事实上,最近的文献表明,这些衍生品通过与秋水仙碱位点结合抑制微管的生成,提出了正确的药代动力学性质以及它们在许多细胞系都有能力克服多药耐药性。咪唑类/苯并咪唑调制微管动力学机制的理解对于克服抗癌药物的耐药性和发现新的生物标志物和癌症化疗的靶标的研究是非常重要的。
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
Current Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/0929867322666150114164032 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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