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%).
Jin
G
G
College of Pharmacy, Yanbian University, Yanji, 133000, Jilin, China.
You
Y
Y
Ahn
B
B
D000818:Animals; D000880:Anthraquinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D004195:Disease Models, Animal; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy / Q000401:mortality; D008558:Melphalan / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D008942:Mitoxantrone / Q000737:chemistry*; D014407:Tumor Cells, Cultured
C433943:2-(1-(4-(p-bis(2-chloroethyl)-aminophenyl)-butanoyloxy)methyl)-1,4-dihydroxy-9,10-anthraquinone; C433944:2-(1-(4-(p-bis(2-chloroethyl)aminophenyl)-butanoyloxy)ethyl)-1,4-dihydroxy-9,10-anthraquinone; D000880:Anthraquinones; D000970:Antineoplastic Agents; D004952:Esters; D008942:Mitoxantrone; D008558:Melphalan