Indole molecules as inhibitors of tubulin polymerization: potential new anticancer agents, an update (2013-2015)

Future Med Chem. 2016 Jul;8(11):1291-316. doi: 10.4155/fmc-2016-0047. Epub 2016 Jul 20.

Abstract

Discovery of new indole-based tubulin polymerization inhibitors will continue to dominate the synthetic efforts of many medicinal chemists working in the field. The indole ring system is an essential part of several tubulin inhibitors identified in the recent years. The present review article will update the synthesis, anticancer and tubulin inhibition activities of several important new indole classes such as 2-phenylindoles (28, 29 & 30), oxindoles (35 & 38), indole-3-acrylamides (44), indolines (46), aroylindoles (49), carbozoles (75, 76 & 82), azacarbolines (87) and annulated indoles (100-105).

Keywords: anticancer; carboline; colchicine; design; drug; indole; structure–activity relationship; synthesis; tubulin inhibitors.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Drug Discovery
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Molecular Conformation
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Polymerization / drug effects
  • Tubulin / metabolism*
  • Tubulin Modulators / pharmacology*

Substances

  • Antineoplastic Agents
  • Indoles
  • Tubulin
  • Tubulin Modulators
  • indole