Exploring Synthetic Strategies and Therapeutic Potential of Naphthoquinone Derivatives: A Review

ABSTRACT Naphthoquinone derivatives are increasingly recognized for their wide‐ranging biological activities and relevance in drug discovery. This review outlines recent advances in the synthesis of naphthoquinone compounds, focusing on strategies that enhance their structural diversity and efficiencies. We explored their broad therapeutic potential, including strong antimicrobial effects against both gram‐negative and gram‐positive pathogens and their capacity to overcome microbial resistance. Their antimalarial activity also shows promise, offering new options for the treatment of drug‐resistant species. In oncology, several derivatives have demonstrated selective cytotoxicity against cancer cell lines, with distinct mechanisms supporting their development as anticancer agents. Additionally, their antioxidant properties offer protection against oxidative stress, which has implications for chronic diseases and aging‐related disorders. Emerging data also indicate neuroprotective effects, particularly in Alzheimer's disease, by modulating oxidative stress and neuroinflammation. These findings underscore the versatility of naphthoquinone derivatives as potential leads in multiple therapeutic areas. By compiling synthetic methods and biological insights, this review provides a comprehensive resource to support future research and the development of naphthoquinone‐based drug candidates.