Chromone, A Privileged Scaffold in Drug Discovery: Developments in the Synthesis and Bioactivity

Mini Rev Med Chem. 2022;22(7):1030-1063. doi: 10.2174/1389557521666211124141859.

Abstract

Chromones are the class of secondary metabolites that broadly occur in the plant kingdom in a noticeable quantity. This rigid bicyclic system has been categorized "as privileged scaffolds in compounds" in medicinal chemistry. Their wide biological responses have made them an important moiety in a drug discovery program. This review provides updates on the various methods of synthesis of chromones and biological applications in medicinal chemistry. Various synthetic strategies for the construction of chromones include readily available phenols, salicylic acid and its derivatives, ynones, chalcones, enaminones, and 2-hydroxyarylalkylketones as starting materials. Synthesis of chromones by using metal, metal-free, nanomaterials and different other catalysts is herein included. Details of diverse biological activities of chromone derviatives, such as anti-cancer, antimicrobial, anti-viral, anti-inflammatory, antioxidant, as Monoamine Oxidase-B (MAO-B) inhibitors, anti- Alzheimer's agents, anti-diabetic agents, having antihistaminic potential, and acting as antiplatelet agents, are discussed.

Keywords: Chromones; anti-cancer; anti-diabetic; anti-viral; antimicrobial; synthetic transformation.

Publication types

  • Review

MeSH terms

  • Chromones* / pharmacology
  • Drug Discovery
  • Humans
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / pharmacology
  • Neoplasms*
  • Structure-Activity Relationship

Substances

  • Chromones
  • Monoamine Oxidase Inhibitors
  • Monoamine Oxidase