A novel metabolite containing sulfur, fusaodavinvin (1), was isolated from an endophytic fungus Fusarium sp.(CTGU-ZL-34), together with seven known compounds 2-8, and their structures were elucidated by NMR spectroscopy and MS. This is the first record of 3-(2R-hydroxyl-1-one-propane)-indole (compound 2) from nature. The isolated compounds were evaluated using the A549, Hep G2, Caski and MCF-7 cell lines by the MTT method, and compound 1 displayed significant inhibiting activity of four cancer cell lines with IC50 values of 11.5, 15.3, 15.2 and 60.5 microg/mL, respectively. However, compound 2 displayed no significant anticancer activity to the above four cancer cell lines.