Antitumor activities of newly synthesized N4-acyl-1-beta-D-arabinofuranosylcytosine.
New derivatives of 1-beta-D-arabinofuranosylcytosine were synthesized and their antitumor activities were tested against mouse leukemia L1210. Among the 50 compounds investigated, a series of N4-acyl derivatives with long-chain saturated fatty acids were found to be highly active. The most active derivatives were N4-stearoly-1-beta-D-arabinofuranosylcytosine, which was administered in the form of suspension, and N4-behenoyl-1-beta-D-arabinofuranosylcytosine given in the form of solution. They were superior to the parent compound, 1-beta-D-arabinofuranosylcytosine, in that smaller dosages exhibited strong activities regardless of the treatment schedule, and they were also resistant to cytidine deaminase.
D000215:Acylation; D000818:Animals; D003561:Cytarabine / Q000031:analogs & derivatives* / Q000627:therapeutic use; D003564:Cytidine Deaminase / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005227:Fatty Acids / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy*; D051379:Mice; D013229:Stearic Acids / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D005227:Fatty Acids; D013229:Stearic Acids; D003561:Cytarabine; D003564:Cytidine Deaminase