Biological Activity and Therapeutic Potential of Coumarin Derivatives: A Comprehensive Review.

Abstract

Coumarins, naturally occurring benzopyrones, have garnered significant attention due to their diverse pharmacological activities and therapeutic potential. Derived from natural sources and synthetic routes such as the Perkin and Pechmann reactions, these compounds exhibit a broad spec-trum of biological activities, including antioxidant, anti-inflammatory, antimicrobial, anticancer, an-tidiabetic, and neuroprotective effects. The structure-activity relationship of coumarins highlights the critical role of substitutions at specific positions on the benzopyrone ring, enhancing their efficacy and selectivity. Notable applications include anticancer activities, with coumarin derivatives inhibit-ing tumor growth and inducing apoptosis in breast cancer and melanoma cells, and neuroprotection, particularly in Alzheimer's and Parkinson's diseases, through acetylcholinesterase inhibition and β-amyloid modulation. Additionally, coumarins show promise in combating drug-resistant pathogens and oxidative stress. Despite their potential, challenges such as toxicity and bioavailability remain. Future research should focus on optimizing coumarin scaffolds and advancing clinical evaluations to establish their role as next-generation therapeutic agents.