Eight esters of 2-(1-hydroxyalkyl)-1, 4-dihydroxy-9, 10-anthraquinone with melphalan were prepared and tested for their antitumor activity (S-180) and cytotoxicity. 2-{1-[4-(p-Bis (2- chloroethyl)-aminophenyl)-butanoyloxy] methyl}-1, 4-dihydroxy-9, 10-anthraquinone and 2- {1-[4-(p-bis (2-chloroethyl)-aminophenyl)-butanoyloxy] ethyl}-1, 4-dihydroxy-9, 10- anthraquinone showed remarkable antitumor activity (T/C, 265 and 272%).