Cycloartane triterpenoids, 2',24-O-diacetylisodahurinol-3-O-α-L-arabinopyranoside, 24-O-acetylisodahurinol-3-O-α-L-arabinopyranoside, 12β-hydroxy-25-anhydrocimigenol, cimigenol-12-one, 12β-hydroxy-15-deoxycimigenol, 2'-O-acetyl-24-epi-cimigenol-3-O-α-L-arabinopyranoside, 2'-O-acetylcimigenol-3-O-β-D-xylopyranoside, 25-anhydrocimigenol-3-O-α-L-arabinopyranoside, 2',23-O-diacetylshengmanol-3-O-α-L-arabinopyranoside, and 2',24-O-diacetyl-25-anhydrohydroshengmanol-3-O-α-L-arabinopyranoside, together with eight known compounds, were isolated from aerial parts of Cimicifuga foetida. Their structures were determined by application of spectroscopic analyses and chemical methods. Biological evaluation of the compounds against human HL-60, SMMC-7721, A549, SK-BR-3, and PANC-1 cell lines indicated that three of these compounds exhibited broad-spectrum and moderate cytotoxic activities, with IC₅₀ values ranging from 6.20 to 22.74 μM. By comparing previous cytotoxic testing data and bioassay results from this study, preliminary structure-activity relationships of compounds with a c imigenol-skeleton can be proposed.