Esters of chlorambucil with 2-substituted 1,4-dihydroxy-9,10-anthraquinones as multifunctional anticancer agents.
Novel twelve esters of chlorambucil with 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone were synthesized and tested for their antitumor activity in mice bearing S-180 ascitic cells as well as cytotoxic activity against L1210 cells. Eight of them were highly cytotoxic on L1210 cells (ED(50), <6 microg mL(-1)) and derivatives 1 and 12 (T/C, 200 and 205%) appeared more active in vivo than chlorambucil (T/C, 168%).
Jin
G Z
GZ
College of Pharmacy, Yanbian University, Yanji, Jilin 133000, People's Republic of China.
You
Y J
YJ
Kim
Y
Y
Nam
N H
NH
Ahn
B Z
BZ
D000818:Animals; D000880:Anthraquinones / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002699:Chlorambucil / Q000737:chemistry* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D007939:Leukemia L1210; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D012513:Sarcoma, Experimental / Q000188:drug therapy / Q000401:mortality; D013329:Structure-Activity Relationship
D000880:Anthraquinones; D000970:Antineoplastic Agents; D002699:Chlorambucil