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Five terpenes (1~5), three fatty acids (6~8), two sterols (9 and 11), and a monogalactosyldiacyl glycerol (10) were isolated from the methylene chloride extract of the aerial part of Cirsium setidens. Their chemical structures were determined to be a-tocopherol (1), 25-hydroperoxycycloart- 23-en-3b-ol (2), 24-hydroperoxycycloart-25-en-3b-ol (3), mokko lactone (4), transphytol (5), 9, 12, 15-octadecatrienoic acid (6), 9, 12-octadecadienoic acid (7), hexadecanoic acid (8), acylglycosyl b-sitosterol (9), (2 R)-1, 2-O-(9z, 12z, 15z-dioctadecatrienoyl)-3- O-b-Dgalactopyranosyl glycerol (10) and b-sitosterol glucoside (11) by spectral evidences. Compound 3 exhibited significant cytotoxic activity against five human cancer cell lines with its ED50 values ranging from 2.66 to 11.25 mM.