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

Research output: Contribution to journalReview articlepeer-review

7 Scopus citations

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.

Original languageEnglish
Pages (from-to)2329-2352
Number of pages24
JournalCurrent Medicinal Chemistry
Volume25
Issue number20
DOIs
StatePublished - 2018
Externally publishedYes

Keywords

  • Antimitotic activity
  • Colchicine binding site
  • Cytotoxic activity
  • Phenstatins
  • Structure-activity relationship
  • Tubulin polymerization inhibition

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