Tyrosol (Tyr), hydroxytyrosol (TH), and 3,4-Dihydroxyacetophenone (3,4-DHAP) are three phenolic compounds naturally present in plants that have attracted considerable research attention due to their potent antioxidant, anti-inflammatory, anticancer, and cardiovascular protective properties. In recent years, mounting evidence has indicated that these phenolic compounds hold broad potential in both disease prevention and treatment. This paper reviews the chemical structures and synthetic methods of Tyr, HT, and 3,4-DHAP, as well as their multifaceted effects on human health, particularly their roles and mechanisms in antioxidation, anti-inflammation, cardiovascular protection, neuroprotection, and anticancer activity. In addition, this paper explores the future prospects of these compounds and the current challenges associated with their application—such as low bioavailability and long-term safety concerns—and proposes directions for further investigation.