Recent Developments on Phenstatins as Potent Antimitotic Agents.

Xing Chen, Shi-Meng Wang, Gajjela Bharath Kumar, Grant A L Bare, Jing Leng, Syed Nasir Abbas Bukhari, Hua-Li Qin

Journal: Current medicinal chemistry 2018;25(20):2329-2352

PMID: 29110592

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.

Copyright© Bentham Science Publishers; For any queries, please email at [email protected].

Address: 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.; Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Sakaka2014, Saudi Arabia.

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