酚抑制素作为强力抗真菌药的研究进展

Title:Recent Developments on Phenstatins as Potent Antimitotic Agents

Volume: 25 Issue: 20

关键词: 结构-活性关系，细胞毒性活性，抗核活性，微管蛋白聚合抑制，秋水仙素结合位点，苯他汀。

摘要: Background: 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.

Objective: 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.

Methods: 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.

Conclusion: 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.

Cite this article as:

Recent Developments on Phenstatins as Potent Antimitotic Agents, Current Medicinal Chemistry 2018; 25 (20) . https://dx.doi.org/10.2174/0929867324666171106162048