Chalcones and Flavones as Multifunctional Anticancer Agents- A Comprehensive Review

Background: Chalcone and flavone moieties play an important role in medicinal chemistry for the development of potential therapeutic agents. These two derivatives serve a wide range of applications in recent studies and are promising lead molecules for the synthesis of compounds with vast therapeutic utility for many diseases, particularly for cancer therapy. Objective: The present review focused on the fact that chalcone and flavone derivatives possess an interesting spectrum of anticancer activities and their representative mechanisms of action for antitumor therapy. Chalcone and flavones have potential in vitro and in vivo anticancer activity on multiple targets with different mechanisms, including topoisomerase inhibition, MDR channel inhibition Targeting NF-kB pathway, Serine/threonine protein kinase inhibition, PRAP1 inhibition, tubulin polymerase inhibition, Aromatase inhibition, cell cycle disruption, apoptosis inducing, immunomodulatory and inflammation mediatory mechanism. The advantage of chalcone and flavone scaffolds is their convenient synthetic methods and wide clinical potential. Methods: We have scrutinized and reviewed 60 research articles published in different databases in recent years highlighting chalcones and flavones with different anticancer activities and evaluated their binding interactions in docking studies and potency in in vitro studies. Substituted chalcones and flavones with various heterocyclic nuclei and aliphatic and aromatic side chains are discussed. A thorough investigation on the mechanism by which each flavone and chalcone exerted its specific anticancer activity was done and is reviewed. Results: It was seen that research conducted on chalcones and flavones proved it as a privileged structure with multifunctional anticancer activity. More exploration of these molecules will provide newer cancer therapeutic agents with less toxicity. Conclusion: The review will be helpful for the wide variety of scientific community doing research on these versatile molecules.