A series of 3-aryl-7-propenoates including cinnamates, (E)-methyl/ethyl 3-[2-(1, 1-dimethoxy-5,8-dione)naphthalenyl]-2- propenoates (8ba, 8bb) and (E3)-methyl/ethyl 3-[2-(1,4-dihydroxy-9,10-dione)anthracenyl]-2-propenoates (9aa, 9ab) was synthesized and evaluated for antitumor cytotoxicity. It was found that the or ortho- or para-dihydroxy functionality on the aryl ring was essential for the cytotoxicity of cinnamates. Compounds 8ba, 8bb and 9aa, 9ab showed potent cytotoxicity against various tumor cell lines. (C) 2001 Elsevier Science Ltd. All rights reserved.