Title:Recent Developments on Phenstatins as Potent Antimitotic Agents
VOLUME: 25 ISSUE: 20
Author(s):Xing Chen , Shi-Meng Wang , Gajjela Bharath Kumar, Grant A.L. Bare, Jing Leng, Syed Nasir Abbas Bukhari* and Hua-Li Qin*
Affiliation:Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070, Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070
Keywords:Structure-activity relationship, Cytotoxic activity, Antimitotic activity, Tubulin polymerization inhibition,
Colchicine binding site, phenstatins.
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.
