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May 31, 20260 citationsOpen Access

Recent Progress in Chalcone Derivatives: Synthetic Strategies, Pharmacological Activities and Molecular Insights

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NPNeha Pisal*

Key Points

  • The aim is to summarize advancements in chalcone derivatives concerning their synthesis and pharmacological potential.
  • Review of conventional and modern synthetic approaches for chalcone derivatives.
  • Examination of biological activities and mechanisms of action of chalcones.
  • Analysis of structure-activity relationships (SAR) and the impact of substituents on properties.
  • Chalcone derivatives display diverse biological activities including antimicrobial and anticancer effects.
  • Modern synthetic techniques improve reaction efficiency and environmental sustainability.
  • Structural insights enhance understanding of ligand-target interactions supporting rational drug design.

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.

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Cite This Study

Neha Pisal* (2026) studied this question.

synapsesocial.com/papers/6a1bd1745783ba022b6fd11ehttps://doi.org/10.5281/zenodo.20444912
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