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KMID : 0370219880320050334
Yakhak Hoeji
1988 Volume.32 No. 5 p.334 ~ p.339
Study on Prodrugs of 1-¥â-D-Arabinofuranosylcytosine


Abstract
AraC-5¢¥-methylthioacetate (araC-MTA, 1) and araC-5¢¥-butylthioacetate (araCBTA, 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.
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