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The objectives of the present study were to isolate active compounds from the stems of Ficus foveolata, and to investigate their cytotoxic activity against several cancer cell lines (MCF-7, HT-29, KB and HeLa cells) using Sulforhodamine B (SRB) assay. Phytochemical study of the stem extract of F. foveolata led to the isolation of four known compounds including flavifloramide B (1), foveolatamide (2), N-trans-feruloyltyramine (3) and N-trans-grossamide (4). Their structure determination was elucidated by spectroscopic analysis (NMR and MS) and compared with previously reported data. The compounds were then investigated for their cytotoxic activity. Among the tested compounds, the compounds 3 and 4 exhibited cytotoxic effect against MCF-7, whereas the compounds 1 and 2 was inactive in all tested cell lines. Compound 4 showed the strongest cytotoxic activity against MCF-7 with IC50 value 1.70 µg/mL, whereas compound 3 showed moderate activity with IC50 value 4.98 µg/mL. Camptothecin (IC50=0.00116 µg/mL) was used as a positive control. Moreover, the compounds 3 and 4 did not show any cytotoxicity with normal cell at the concentration of 10 µg/mL.