Aaptamine (8,9-dimethoxy-1H-benzo[de][1,6]naphthyridine), an alkaloid obtained from marine sponges of the genus Aaptos (Demospongiae, Suberitida, Suberitidae), has attracted significant attention as a promising scaffold for the development of antioxidant, antibacterial, and anticancer agents. This review offers an extensive overview of updated research on aaptamine, focusing on its multifaceted pharmacological properties. The antioxidant potential of aaptamine reflects its potential ability for use in the DPPH free radical scavenging assay, for suppressing ROS, and subsequently deactivating the MAPK and AP-1 signaling pathway. Moreover, it demonstrates notable antibacterial activity against pathogenic bacteria, including mycobacterial active and dormant states, making it a potential candidate for combating bacterial infections. Additionally, aaptamine shows promising anticancer activity by inhibiting cancer cell proliferation, apoptosis induction, and suppressing tumor growth through various signaling pathways, including the regulation of PTEN/PI3K/Akt and CDK2/4, and the regulation of cyclin D1/E in cell cycle arrest. The unique chemical structure of aaptamine offers opportunities for structural modifications aimed at enhancing its antioxidant, antibacterial, and anticancer activities. The exploration of aaptamine as a scaffold in the development of novel therapeutic agents offers great promise for addressing various challenges associated with oxidative stress, bacterial infections, and cancer. This article underscores the potential of aaptamine as a valuable marine-derived scaffold in the fields of antioxidant, antibacterial, and anticancer therapy.