Acridine derivatives. III. Preparation and antitumor activity of the novel acridinyl-substituted uracils.
In an investigation of a new class of deoxyribonucleic acid (DNA)-intercalating antitumor agents, novel acridinyl-substituted uracils have been synthesized and evaluated for activity against L1210 leukemia in vivo, and against bacteria and fungus. These compounds were prepared by the novel enamine reaction between 9-chloroacridines and 6-aminouracils. The positional effects of substituents on the acridine ring showed that compounds bearing electron-withdrawing groups at the 3- or 6-position of the acridine ring were the most active.
Kimura
M
M
Okabayashi
I
I
Kato
A
A
D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology; D000677:Amsacrine / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D051379:Mice; D008811:Mice, Inbred DBA; D013329:Structure-Activity Relationship; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D000166:Acridines; D000970:Antineoplastic Agents; D000677:Amsacrine; D014498:Uracil