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*, Hua-Li Qin*.

Journal Name: Current Medicinal Chemistry

Volume 25 , Issue 20 , 2018

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Abstract:

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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Article Details

VOLUME: 25
ISSUE: 20
Year: 2018
Page: [2329 - 2352]
Pages: 24
DOI: 10.2174/0929867324666171106162048
Price: $58

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