Studies of the ethyl acetate extract bark extract of Olea ferruginea led to the isolation of one new compound Ferruginan A (1) in addition to two known compounds, Ferruginan (2) and cycloolivil (3). Structures of the isolated compounds were confirmed by mass spectrometry (MS) and NMR spectral data. The ethyl acetate fraction and compounds (1–3) were evaluated against breast cancer cell line (MCF-7) and as antioxidants using the free radical scavenging assay. Results revealed that compound 2 exhibits significant antioxidant activity with an I C 50 value of 21.74 μg/mL. In addition, the ethyl acetate fraction showed good cytotoxic activity (79.31% inhibition at 250 μg/mL), whereas compounds 1–3 exerted mild cytotoxic activity ( I C 50 = 8.03 – 12.01 μ g / mL ) as compared to the standard ( I C 50 = 4.41 μ g / mL ) against MCF-7. Docking studies suggested that antioxidant activity is due to the chelation of compounds with copper present in the active site of tyrosinase. These results suggest that the extract exhibits considerable antioxidant activity, and the isolated compounds exert moderate anticancer activity.