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Often, these natural substances necessitate structural alterations to yield promising lead compounds. Chalcones, characterized by their \u03b2\u2010unsaturated carbonyl aromatic ketone structure, are prevalent in plant life and serve as fundamental scaffolds for the biosynthetic precursors of flavonoids and isoflavones. Due to their straightforward synthesis and extensive spectrum of biological effects, chalcones have found extensive application in medicinal chemistry. Chalcone analogs have demonstrated significant potential for drug discovery and development, as structural modifications can both amplify pharmacological efficacy and effectively mitigate toxic side effects. This paper endeavors to delve into the applications of chalcones in the structural modification of natural products, providing a theoretical foundation for future endeavors in derivatization and drug development. 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