Advancements in synthetic methodologies and biological applications of lawsone derivatives.

Abstract

2-Hydroxy-1,4-naphthoquinone, widely recognized as lawsone, is a natural dye obtained from the henna plant (Lawsonia inermis), known for its biological activity and diverse applications in biochemistry and analytical chemistry. As a versatile precursor, it plays a crucial role in synthesizing a wide range of structurally diverse and bioactive molecular scaffolds. This review highlights recent progress in the development of lawsone derivatives, emphasizing their extensive biological activities, such as anticancer, antimicrobial, antioxidant, antimalarial, and metabolic enzyme-targeting activities, as well as their structure-activity relationships. Remarkably, this is the first detailed exploration covering both the biological activities and chemical synthesis of significant lawsone derivatives from 2016 to the present.