Benzimidazole Scaffold as Anticancer Agent: Synthetic Approaches and Structure-Activity Relationship

Arch Pharm (Weinheim). 2017 Jun;350(6). doi: 10.1002/ardp.201700040. Epub 2017 May 22.

Abstract

Cancer, also known as malignant neoplasm, is a dreadful disease which involves abnormal cell growth having the potential to invade or spread to other parts of the body. Benzimidazole is an organic compound that is heterocyclic and aromatic in nature. It is a bicyclic compound formed by the fusion of the benzene and imidazole ring systems. It is an important pharmacophore and a privileged structure in medicinal chemistry. According to the World Health Organisation (2015 survey), one in six deaths is due to cancer around the globe, accounting for 8.8 million deaths of which 70% of the cases were from low- and middle-income countries. In the efforts to develop suitable anticancer drugs, medicinal chemists have focussed on benzimidazole derivatives. This review article covers the current development of benzimidazole-based anticancer agents along with the synthetic approaches and structure-activity relationships (SAR).

Keywords: Alkylating agents; Anticancer; Benzimidazole; Topoisomerase inhibitors; Tubulin inhibitors.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology*
  • Cell Proliferation / drug effects
  • DNA Topoisomerases / metabolism*
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Topoisomerase Inhibitors / chemical synthesis
  • Topoisomerase Inhibitors / chemistry
  • Topoisomerase Inhibitors / pharmacology*

Substances

  • Antineoplastic Agents
  • Benzimidazoles
  • Topoisomerase Inhibitors
  • benzimidazole
  • DNA Topoisomerases