抗有丝分裂剂
微管蛋白
化学
组合化学
前提
细胞毒性
计算生物学
立体化学
微管
计算机科学
体外
生物化学
生物
细胞生物学
哲学
语言学
作者
Xing Chen,Shi‐Meng Wang,G. Bharath Kumar,Grant A. L. Bare,Jing Leng,Syed Nasir Abbas Bukhari,Hua‐Li Qin
标识
DOI:10.2174/0929867324666171106162048
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.
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