Abstract: Based on intercalation mechanism, twelve daunomycin and adriamycin analogues have been synthesized. Esterification of daunomycinone with appropriate MOZ-amino acid was accomplished in the presence of benzenesulfonyl chloride or DCC to afford intermediates (23～28). After cleavage of the protective groups compounds (5～10) and (14～16) were obtained. Bromination of (8), (9) and (10), followed by hydrolysis, gave adriamycin analogues(11), (12) and (13).In preliminary biological tests against HeLa cell and human gastric carcinoma SGC-7901 cell line in vitro and against L-7712 leukemia in mice most of these compounds showed antitumor activity. The trans-form analogues (9) and (12) were more active than the cis-form isomers (8) and (11). The adriamycin analogues(11), (12) and (13) were more active than the respective daunomycin analogues (8), (9) and (10) and compound (12) showed to be the most active.