Indole derivatives (2010-2020) as versatile tubulin inhibitors: synthesis and structure-activity relationships

Future Med Chem. 2021 Oct;13(20):1795-1828. doi: 10.4155/fmc-2020-0385. Epub 2021 Sep 1.

Abstract

Tubulin inhibitors are conjugates that interfere with the dynamic equilibrium of the polymerization and depolymerization of microtubules. Among all the reported conjugates, indole moiety is one of the most significant classes for the development of new drug candidates for cancer therapy. Due to their presence in a wide range of natural as well as synthetic antitubulin agents, indole has become a versatile scaffold in research, and various synthetic and semisynthetic indole-based antitubulin agents have been identified and reported. The present article focuses on the reported indole-based tubulin inhibitors of synthetic origin from last the decade. Synthesis, structure-activity relationships and biological activities of synthetic indole derivatives along with brief updates on their antitubulin activity are presented.

Keywords: IC50; anticancer; antiproliferative; colchicine; combretastatin; indole; tubulin.

Publication types

  • Review

MeSH terms

  • Dose-Response Relationship, Drug
  • Humans
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Molecular Structure
  • Structure-Activity Relationship
  • Tubulin / metabolism*
  • Tubulin Modulators / chemistry
  • Tubulin Modulators / pharmacology*

Substances

  • Indoles
  • Tubulin
  • Tubulin Modulators