ANTITUMOR ACTIVITIES OF NEWLY SYNTHESIZED N4-ACYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE

  • 1 January 1976
    • journal article
    • research article
    • Vol. 36  (8) , 2726-2732
Abstract
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 highly active. The most active derivatives were N4-stearoyl-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.