While natural products have undeniably played a crucial role in drug discovery, challenges such as limited availability and complex synthesis methods have hindered the identification of lead compounds. At the core of numerous natural and synthetic compounds, each displaying distinct biological behaviours, lies the foundational structure of 2-quinolinone. Compounds with this structural motif exhibit a broad range of effects in different tissues. Furthermore, specific members showcase therapeutic potential for various disorders. Despite the significance of these compounds, the current review literature has not provided a comprehensive overview, underscoring the essential contribution of this article in exploring their biological functions. This study examines the biological activity of selected 2-quinolinone alkaloids across diverse organisms, unveiling their potential as a source of innovative bioactive natural products.