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Abstract <p>Lawsone (2-hydroxy-1,4-naphthoquinone) has emerged as a privileged scaffold for the construction of bioactive heterocycles with applications spanning antimicrobial, antioxidant, antimalarial, anticancer, and antiplatelet therapies. This review distills advances in both classical (nucleophilic addition, cyclization) and modern (C–H activation, multicomponent, photoinduced) synthetic routes under green chemistry protocols, as well as functionalization strategies that modulate biological activity. Structure–activity relationship studies indicate that strategically incorporating lipophilic chains, aromatic groups, and heterocyclic rings improves target binding and enhances cellular potency. The growing portfolio of lawsone–metal complexes further extends therapeutic potential through dual antimicrobial and anticancer mechanisms. Despite these promising findings, comprehensive <i>in vivo</i> validation, metabolic stability, and toxicity assessments remain scarce. Future efforts should prioritize detailed SAR studies, advanced delivery platforms, and combinatorial regimens to accelerate the clinical translation of lawsone-derived drug candidates.</p>

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Lawsone-Derived Heterocycles: Synthetic Strategies, Structure–Activity Relationships, and Therapeutic Applications

  • 期刊论文

  • 发表日期：

    2026年5月5日

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  • J. P. Sonawane,
  • V. S. Patil,
  • V. K. Suryawanshi,
  • S. S. Nandre,
  • P. M. Raotale,
  • S. R. Patil

摘要

Abstract

Lawsone (2-hydroxy-1,4-naphthoquinone) has emerged as a privileged scaffold for the construction of bioactive heterocycles with applications spanning antimicrobial, antioxidant, antimalarial, anticancer, and antiplatelet therapies. This review distills advances in both classical (nucleophilic addition, cyclization) and modern (C–H activation, multicomponent, photoinduced) synthetic routes under green chemistry protocols, as well as functionalization strategies that modulate biological activity. Structure–activity relationship studies indicate that strategically incorporating lipophilic chains, aromatic groups, and heterocyclic rings improves target binding and enhances cellular potency. The growing portfolio of lawsone–metal complexes further extends therapeutic potential through dual antimicrobial and anticancer mechanisms. Despite these promising findings, comprehensive in vivo validation, metabolic stability, and toxicity assessments remain scarce. Future efforts should prioritize detailed SAR studies, advanced delivery platforms, and combinatorial regimens to accelerate the clinical translation of lawsone-derived drug candidates.