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Triazine compounds have become crucial entities in the pharmaceutical field due to their remarkable structural diversity and wide range of biological activities. This review explores their prominent role in drug discovery and development, focusing on their efficacy as potent anticancer, antiviral, antimicrobial, and antioxidant agents. Recent advances in synthetic methodologies using various starting materials, such as nitrile, biguanide, bromoester, arylamine, and cyanide chloride, are reviewed, along with their implications for improved pharmacological properties, including anticancer, antibacterial, antioxidant, anti-inflammatory, and antimicrobial effects. In addition, the structure-activity relationship of triazine derivatives is explored, offering insight into the key structural features that contribute to their therapeutic potential. This relationship plays an essential role in optimizing their efficacy as therapeutic agents, helping to guide the development of more effective drugs with improved pharmacological profiles.