Study on Prodrugs of $1-{\beta}-D-Arabinofuranosylcytosine$ -Preparation of araC-5'-Alkylthioacetates and Evaluation of their Physical-chemical Properties and Antitumor Activities-

$1-{\beta}-D-Arabinofuranosylcytos$의 Prodrug 연구 -AraC-5'-Alkylthioacetates 합성 및 그들의 물리.화학적 성질과 항암작용 시험-

AraC-5'-methylthioacetate (araC-MTA, 1) and araC-5'-butylthioacetate (araC-BTA, 2) were prepared and their physical and chemical properties and in vivo antitumor activities were examined. Both compounds were found to have higher partiton coefficients (n-hexanol/water) than their parent araC and to be hydrolyzed to araC within an hour in mouse plasma and ascitic fluid solutions. In in vivo antitumor activity test they showed similar potency to araC, which were assumed due to too quick hydrolyses of them to parent in the body fluid.