Benzopyran Derivatives as Emerging Anticancer Agents: Advances in Synthesis, SAR Insights, and Therapeutic Potential

Abstract Benzopyran derivatives have garnered significant attention in medicinal chemistry due to their structural diversity and potent anticancer properties. This review presents a comprehensive analysis of recent advancements in the synthesis of benzopyran analogs using both conventional and modern strategies, such as one‐pot, microwave‐assisted, and ultrasound‐mediated approaches. Emphasis is placed on structure–activity relationship trends, highlighting how specific substituents influence interactions with critical molecular targets, including tubulin, estrogen receptors, and kinases. Additionally, the role of benzopyrans in modulating apoptosis, disrupting cell cycle progression, and overcoming multidrug resistance is critically evaluated. Despite promising preclinical outcomes, further research is essential to enhance tumor specificity, reduce toxicity, and facilitate clinical translation. Overall, benzopyran scaffolds offer a versatile platform for the development of next‐generation anticancer therapeutics.