The Annonaceae is one of the plant families with members that are credited with numerous pharmacological functions. Among the group of compounds responsible for these bioactivities are the ent-kaurane diterpenoids. The ent-kauranes are a group of 20-Carbon, tetracyclic diterpenoids that are widely distributed in other plant families including the Annonaceae family. This mini-review focuses mainly on the ent-kaurane diterpenoids isolated from the Annonaceae family, delineates the various biological activities of these compounds, and highlights the research gaps that exist for further scientific scrutiny.