In search for plant-derived anticancer compound, it was found that the chloroform extracts obtained from the whole plant of Carpesium rosulatum MIQ. (Compositae) exhibited significant anticancer activity against human tumor cell line, A549, SK-OV-3, SK-MEL-2, XF-498, HCT-15. The structures and stereochemistry of these compounds were established on the basis of analysis of spectra including mp, [alpha](D)(25), IR, UV, EI-MS, MS, (1)H-NMR, (13)C-NMR and some chemical transformations as follows: 1 (4 beta, 10 alpha-dihydroxy-guaia-8 alpha, 12-olide), 2 (4 beta, 10 alpha-dihydroxy-1(2), 11(13)-guaiadien-8 alpha, 12-olide), 3 (3 beta, 8 beta-dihydroxy-1 alpha, 5 alpha-guaian-10(14)-ene-6 alpha, 12-olide). Anticancer activity of compounds obtained from C. rosulatum MIQ. on five tumor cells line was evaluated by procedure of SRB methods. 2 significantly effects to the five human tumor cell lines.