N4-BEHENOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE AS A POTENTIAL NEW ANTITUMOR AGENT

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  • 1 January 1977
    • journal article
    • research article
    • Vol. 37  (8) , 2481-2486
Abstract
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 in treating mouse L1210 leukemia. 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 was 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. 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.