Natural products are sources of secondary metabolites with various biological activities. This review highlights the promising potential of the Annonaceae family, a large clade of flowering plants with 107 genera and over 2300 species. Known for their vast pharmacological activities, several genera and species within this family are considered excellent sources of bioactive molecules due to the diversity of their secondary metabolites. Chemical investigations have revealed the presence of alkaloids, mainly isoquinolinic alkaloids, phenolic compounds, terpenoids, lactones, and acetogenins. The Annonaceae family exhibits anti-inflammatory, insecticidal, antimicrobial, leishmanicidal, cytotoxic, antitumor, trypanocidal, antioxidant, gastroprotective, and antimalarial activities. However, most studies focus on plant extracts and essential oils, with few isolated molecules and mechanisms of action identified. Investigating the biological activity of isolated compounds is crucial for new drug discovery. This review also compiles important information for the pharmaceutical and agricultural industries.