N4-Behenoyl-1-beta-D-arabinofuranosylcytosine as a potential new antitumor agent.
N4-Acyl-1-beta-D-arabinofuranosylcytosines, which are lipophilic antitumor analogs of 1-beta-D-arabinofuranosylcytosine, were dissolved by the use of a detergent, HCO-60, and the differences in the antitumor activities when the drugs were administered in the forms of solution or suspension were compared. N4-Stearoyl-1-beta-D-arabinofuranosylcytosine (NSC 201290), which was the most active compound when administered as an aqueous suspension, diminished in its activities after it had been dissolved into a clear solution, whereas N4-behenoyl-1-beta-D-arabinofuranosylcytosine (NSC 239336) exhibited activities superior to those of the parent compound 1-beta-D-arabinofuranosylcytosine when administered as a solution. Moreover, the high efficacy of this compound was long lasting in the host animal, regardless of the treatment schedules or the presence of the 1-beta-D-arabinofuranosylcytosine-inactivating enzyme, cytidine deaminase.
D000818:Animals; D000970:Antineoplastic Agents; D002478:Cells, Cultured; D003561:Cytarabine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D003564:Cytidine Deaminase / Q000494:pharmacology; D005260:Female; D006868:Hydrolysis; D007939:Leukemia L1210 / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008811:Mice, Inbred DBA; D012996:Solutions; D013535:Suspensions; D013997:Time Factors
D000970:Antineoplastic Agents; D012996:Solutions; D013535:Suspensions; D003561:Cytarabine; D003564:Cytidine Deaminase