The oleoresins from Copaifera species (copaiba) have been used by native peoples of the Amazon region for thousands of years. These materials have shown remarkable biological activities, including antibacterial, antiparasitic, antineoplastic, and anti-inflammatory activities. Copaiba resins have been distilled to give essential oils that are largely composed of sesquiterpenoids, particularly β-caryophyllene. The resins are also composed of diterpene acids, which are responsible for many of the observed biological activities. Molecular docking of copaiba diterpene acids with documented protein targets has revealed potential mechanisms of activity for these bioactive constituents. Future research to validate the molecular mechanisms of copaiba diterpenoids is encouraged.