Recent developments in tubulin polymerization inhibitors: An overview

Eur J Med Chem. 2014 Nov 24;87:89-124. doi: 10.1016/j.ejmech.2014.09.051. Epub 2014 Sep 16.

Abstract

Microtubules are protein biopolymers formed through polymerization of heterodimers of α- and β-tubulins. Disruption of microtubules can induce cell cycle arrest in G2-M phase and formation of abnormal mitotic spindles. Their importance in mitosis and cell division makes microtubules an attractive target for anticancer drug discovery. A number of naturally occurring compounds such as paclitaxel, epothilones, vinblastine, combretastatin, and colchicines exert their effect by changing dynamics of tubulin such as polymerization and depolymerization. During past few years, rapid development of the novel tubulin polymerization inhibitors has been witnessed. Diverse classes of chemical compounds from the natural as well as from the synthetic origin have been extensively studied. This review highlights the various classes of synthetically derived chemical compounds those have been reported in last few years as potential tubulin polymerization inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the brief SAR studies. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds to inhibit the tubulin polymerization.

Keywords: Disruption of microtubules; Microtubules; Tubulin polymerization; Tubulin polymerization inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Microtubules / drug effects*
  • Mitosis / drug effects*
  • Polymerization / drug effects*
  • Tubulin / metabolism*
  • Tubulin Modulators / pharmacology*

Substances

  • Tubulin
  • Tubulin Modulators