RECENT PROGRESS IN CHALCONE DERIVATIVES: SYNTHETIC STRATEGIES, PHARMACOLOGICAL ACTIVITIES AND MOLECULAR INSIGHTS
Neha Pisal*, Atharva Londhe, Muskan Shaikh, Arpita Pimparkar, Vijay Waghmare, Mrs. Sapana Nagare
ABSTRACT
Chalcones represent an important class of flavonoid-related compounds that occur in both natural and synthetic forms. They are structurally characterized by an α, β? unsaturated carbonyl framework, which plays a crucial role in their chemical reactivity and pharmacological potential.[6,7] These compounds are widely distributed in plants and are involved in various physiological processes, including defense mechanisms and metabolic functions.[13] Owing to their simple structure and ease of modification, chalcones have gained significant attention as promising scaffolds in medicinal chemistry and drug discovery.[17,21] Conventional synthetic approaches such as Claisen-Schmidt condensation remain widely used; however, recent advancements have introduced modern techniques including micro- assisted synthesis and green chemistry approaches that improve reaction efficiency, reduce time, and minimize environmental impact.[1,2,14] Chalcone derivatives exhibit a wide range of biological activities, including antimicrobial, anti-inflammatory, antioxidant, anticancer, and antitubercular effects. These properties are primarily attributed to the presence of an electrophilic α,β? unsaturated carbonyl group, which facilitates interaction with biomolecular targets such as enzymes and proteins.[6,12] Furthermore, computational approaches such as molecular docking and in silico studies have enhanced the understanding of ligand-target interactions, thereby supporting rational drug design.[60-62] This review provides a comprehensive overview of recent developments in chalcone chemistry, including synthesis, characterization, biological activities, and mechanisms of action. Special emphasis is placed on structure-activity relationship (SAR) and the influence of substituents on biological properties. The future potential of chalcone derivatives in pharmaceutical research is also highlighted.
[Full Text Article] [Download Certificate]

