Esters of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinones with melphalan as multifunctional anticancer agents

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%).