Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, China.
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States.
Curr Med Chem. 2018;25(20):2329-2352. doi: 10.2174/0929867324666171106162048.
Phenstatin and their derivatives display remarkable antiproliferative activity toward a wide variety of preclinical tumor models. Structural simplicity and excellent stability of phenstatins offer a stimulating premise for developing various derivatives with profound antimitotic activity and excellent cytotoxicity.
To do analysis of literature that phenstatins derivatives inhibit tubulin polymerization through their interaction at the colchicine binding site of microtubules and arrest the G2/M phase of the cell cycle. In addition, phenstatin derivatives are undergoing clinical evaluation as vascular targeting/disrupting agents and also exhibit direct antiangiogenic properties.
An organised well designed and appropriately managed search of bibliographic databases for peer-reviewed research literature using a focused review question and inclusion/ exclusion criteria has been done for this article.
In this review article, the synthesis and structure-activity relationships of phenstatin and a wide number of their reported analogues with modifications to ring A, ring B, and to the keto position are discussed in the perspective of medicinal chemistry with proper conclusion.
苯并噻嗪及其衍生物对多种临床前肿瘤模型表现出显著的抗增殖活性。苯并噻嗪结构简单，稳定性好，为开发具有深刻抗有丝分裂活性和良好细胞毒性的各种衍生物提供了一个令人振奋的前提。
通过与微管上的秋水仙碱结合位点相互作用抑制微管聚合，并使细胞周期停滞在 G2/M 期，对文献进行分析。此外，苯并噻嗪衍生物正在作为血管靶向/破坏剂进行临床评估，并且还表现出直接的抗血管生成特性。
本文采用有针对性的综述问题和纳入/排除标准，对同行评议研究文献的书目数据库进行了有组织、精心设计和适当管理的搜索。
在这篇综述文章中，从药物化学的角度讨论了苯并噻嗪及其广泛报道的类似物的合成和构效关系，这些类似物对环 A、环 B 和酮位进行了修饰，并得出了恰当的结论。
