Covering: 2000-2023Cytochalasans are a fascinating class of natural products that possess an intricate chemical structure with a diverse range of biological activities. They are known for their complex chemical architectures and are often isolated from various fungi. These compounds have attracted attention due to their potential pharmacological properties, including antimicrobial, antiviral, and anticancer effects. For decades, researchers have studied these molecules to better understand their mechanisms of action and to explore their potential applications in medicine and other fields. This review article aims to shed light over the period 2000-2023 on the structural diversities of 424 fungal derived cytochalasans, insights into their biosynthetic origins, pharmacokinetics and their promising therapeutic potential in drug discovery and development.