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
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.