Coumarin-containing hybrids and their anticancer activities

Eur J Med Chem. 2019 Nov 1:181:111587. doi: 10.1016/j.ejmech.2019.111587. Epub 2019 Aug 5.

Abstract

Cancer is the second leading cause of death worldwide, and it results in around 9 million deaths annually. The anticancer agents play an intriguing role in the treatment of cancers, while the severe anticancer scenario and the emergence of drug-resistant especially multidrug-resistant cancers create a huge demand for novel anticancer drugs with different mechanisms of action. The coumarin scaffold is ubiquitous in nature and is a highly privileged motif for the development of novel drugs due to its biodiversity and versatility. Coumarin derivatives can exert diverse antiproliferative mechanisms, and some of them such as Irosustat are under clinical trials for the treatment of various cancers, revealing their potential as putative anticancer drugs. Hybridization of coumarin moiety with other anticancer pharmacophores is a promising strategy to reduce side effects, overcome the drug resistance, and may provide valuable therapeutic intervention for the treatment of cancers. Thus, coumarin-containing hybrids occupy an important position in the development of novel anticancer agents. This review aims to summarize the recent advances made towards the development of coumarin-containing hybrids as potential anticancer agents, covering articles published between 2015 and 2019, and the structure-activity relationship together with mechanisms of action are also discussed.

Keywords: Anticancer; Coumarin; Hybrid molecules; Mechanism of action; Structure-activity relationship.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Coumarins / chemistry*
  • Coumarins / pharmacology*
  • Drug Design
  • Drug Discovery
  • Humans
  • Neoplasms / drug therapy*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Coumarins