Anhar Abdel‐Aziem, Salwa A. Elsharabasy, Mariam T. Sayed
ABSTRACT Coumarin (2H‐chromen‐2‐one) and its derivatives represent a significant class of organic compounds, known for their natural occurrence and wide range of pharmaceutical applications. The coumarin scaffold is highly versatile, enabling modifications at various positions on its core structure, often leading to enhanced biological activities, such as antimicrobial, antioxidant, anti‐inflammatory, anticoagulant, antitumor, and enzyme inhibition properties. These modifications not only improve therapeutic potential but also facilitate selective interactions with a variety of biological targets, making coumarin derivatives promising candidates in drug discovery for cancer, neurodegenerative diseases, and metabolic disorders. This review summarizes the various synthetic methods for producing coumarin derivatives, emphasizing the use of different starting materials such as aldehydes, phenols, ketones, carboxylic acids, and reaction conditions to achieve the desired structural modifications. It also highlights the biological importance of these compounds, focusing on their enhanced activities due to structural modifications and their potential in therapeutic applications.