2'-Hydroxycinnamaldehyde (HCA) was isolated from Cinnamomum cassia Blume (Lauraceae) and 2'-benzoyloxycinnamaldehyde (BCA) was prepared by the reaction of HCA and benzoyl chloride. HCA and BCA strongly inhibited in vitro growth of 29 kinds of human cancer cells and in vivo growth of SW-620 human tumor xenograft without the loss of body weight in nude mice. HCA prevented adherence of SW-620 cells to the culture surface but did not inhibit oncogenic K-Ras processing, implying its antitumor mechanisms at the cellular level.