Indolo[2,1-b]quinolin-7(8H)-one derivatives, known as indolonaaphthyridine alkaloids, are a unique class of natural products characterized by their complex molecular structure and diverse biological activities. These alkaloids are primarily found in various plants and fungi, with some species being particularly rich sources. Structurally, they typically consist of an indole ring fused to a quinoline or isoquinoline ring system, which confers them distinctive properties. Indolonaaphthyridine alkaloids have garnered significant attention due to their potential therapeutic applications. Research indicates these compounds exhibit promising activities against a wide range of diseases, including cancer, inflammation, and neurodegenerative disorders. Their structural complexity allows for the possibility of developing highly potent bioactive molecules through targeted modifications. However, their synthesis remains challenging due to the intricate nature of their structure. Due to their multifaceted biological properties, indolonaaphthyridine alkaloids have been extensively studied in academia and industry. They are of particular interest as lead compounds for drug discovery, offering potential avenues for developing new treatments for various ailments.