Canthin-6-one exhibits significant biological activity, making it valuable in pharmaceutical and biomedical research. It shows promising antitumor properties by inhibiting the growth of various cancer cell lines, including those resistant to conventional therapies. Its ability to induce apoptosis and interfere with cell cycle progression supports its potential as a lead compound in anticancer drug development. Additionally, canthin-6-one demonstrates antimicrobial and antiviral effects, particularly against pathogens such as bacteria and certain RNA viruses, suggesting utility in treating infectious diseases. It also possesses anti-inflammatory and neuroprotective activities, which may be leveraged in managing neurodegenerative conditions like Alzheimer’s disease. Due to its broad-spectrum bioactivity, canthin-6-one is actively studied for use in multitarget therapeutic agents and as a scaffold for synthetic optimization in medicinal chemistry.