Advance Therapeutical Use Of Chalcone Derivatives in The Field of Anticancer Drug Discovery

Abstract

Chalcones, a versatile class of open-chain, or close chain flavonoids (1,3diaryl-2-propen-1-ones), have gained significant attention in recent years for their promising role in anticancer drug discovery. Their simple synthetic accessibility, structural flexibility, and ability to interact with multiple molecular targets make them attractive scaffolds in medicinal chemistry. Numerous studies have demonstrated that chalcone derivatives exhibit potent anticancer activity through mechanisms such as induction of apoptosis, disruption of tubulin polymerization, inhibition of angiogenesis, and modulation of signaling pathways including NF-κB, PI3K/Akt, and MAPK. Furthermore, the incorporation of different substituent (methoxy, hydroxyl, halogens, heterocycles) has been shown to enhance selectivity and efficacy against diverse cancer cell lines. Recent advances also highlight the synergistic potential of chalcone-based metal complexes, which often demonstrate superior cytotoxicity compared to free ligands. Computational tools such as molecular docking and density functional theory (DFT) further aid in understanding the structure–activity relationship and predicting binding affinities with cancer-related proteins. This review emphasizes the multifaceted role of chalcone derivatives in anticancer therapy, focusing on their synthetic strategies, mechanistic insights, biological activity, and future prospects in drug development.Chalcone are common simple chemical scaffolds found in many naturally occurring compound. many chalcone derivatives were also prepared due to their convenient synthesis

Keywords: Chalcone derivatives, anticancer therapy, apoptosis, angiogenesis, metal complexes, signaling pathways, computational studies.