Unveiling the Therapeutic Potential of Flavones: A Review on Biological Activities and Mechanisms

Abstract

Flavones, or 2-phenylchromones, are a group of oxygenated heterocyclic compounds belonging to the family of flavonoids. Studying these secondary metabolites has regained interest due to their diverse pharmacological potential, including antioxidant, anticancer, antimicrobial, and anti-inflammatory activities. Some secondary metabolites, such as flavopiridol and riviciclib, have progressed to clinical trials as cyclin-dependent kinase (CDK) inhibitors. This review summarizes recent advances in the study of natural and synthetic flavones, with particular emphasis on their mechanisms of action and structure-activity relationships (SAR). Studies show that flavones have multiple functions, including regulation of oxidative stress, apoptosis, cell cycle arrest, microbial growth, and inflammation. Notably, the chemical modification of the flavone scaffold, particularly phenyl and chromone ring substitutions, affects the potency, selectivity, and therapeutic value and can therefore inform the rational design of drugs. The clinical advancement of flavopiridol and riviciclib demonstrates the potential for translating flavone-based compounds into targeted CDK inhibitors. In this respect, we can consider flavones as a bioactive class of compounds with considerable potential for the development of new drugs. We expect more detailed mechanistic studies with SAR correlation to enable the production of new flavone compounds to broaden the use of these compounds to treat cancer, inflammation, and infectious diseases.