The purification of the MeOH extracts from the aerial parts of Aceriphyllum rossii Engler (Saxifragaceae) using column chromatography furnished fourteen compounds (1 - 14). The chemical structures of the isolated compounds were determined using mainly nuclear magnetic resonance spectra and mass spectrometry. All the isolated compounds were tested for their cytotoxic activity against LH-60, MCF-7 and HeLa cancer cells in vitro using a MTT assay method. Compounds possessing an olean-triterpenoid skeleton entirely exhibit dose dependent cytotoxic activity. These findings partially confirmed the anticancer effect of this medicinal plant, suggesting a further study on the anticancer potential of the triterpenoid structure in compounds from this plant.