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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Recent Developments on Phenstatins as Potent Antimitotic Agents

Author(s): Xing Chen , Shi-Meng Wang , Gajjela Bharath Kumar, Grant A.L. Bare, Jing Leng, Syed Nasir Abbas Bukhari* and Hua-Li Qin*

Volume 25, Issue 20, 2018

Page: [2329 - 2352] Pages: 24

DOI: 10.2174/0929867324666171106162048

Price: $65


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.

Keywords: Structure-activity relationship, Cytotoxic activity, Antimitotic activity, Tubulin polymerization inhibition, Colchicine binding site, phenstatins.

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