Recent advancements of coumarin-based anticancer agents: An up-to-date review

Bioorg Chem. 2020 Oct:103:104163. doi: 10.1016/j.bioorg.2020.104163. Epub 2020 Aug 26.

Abstract

Heading the list of the critical health-related issues worldwide, cancer continues to be a one of the most serious life-threatening diseases. The rate of cancer-related mortality is at alarming level globally because of poor ability of prevention, diagnosis and efficient treatment of cancers. Pertaining to its wide prevalence in many naturally occurring compounds, coumarin as a privileged scaffold is endowed with outstanding anticancer profile. Different classes of coumarin-based anticancer agents that act through diverse mechanisms of action have been comprehensively investigated by many researchers, such as alkylating agents, topoisomerase inhibitors, hormone antagonists, angiogenesis inhibitors, antimitotic agents, apoptosis inducers, human carbonic anhydrase inhibitors, telomerase inhibitors and other mechanisms. Accordingly, medicinal chemists and drug design scientists embarked on exploring diverse coumarin-based derivatives comprehending their potential to develop new efficient anticancer agents. The present review provides an overview of different anticancer classes based on the coumarin scaffold that have been reported since 2015 with particular emphasis on their cellular and enzymatic mechanism of actions.

Keywords: Anticancer; Biological activity; Coumarins; Mechanistic insights; Structure-activity relationships.

Publication types

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

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Coumarins / pharmacology
  • Coumarins / therapeutic use*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Coumarins
  • coumarin