| 摘要 |
PURPOSE: L-type thionucleosides substituent manufactured by substituting no. 2' position are provided which are good for an anticancer drug or antiviral agent(anti-HBV, anti-HSV or anti-HCMV). CONSTITUTION: New thionucleosides(I) useful as an anticancer drug or antiviral agent(anti-HBV, anti-HSV or anti-HCMV) are prepared. In formula(I), R1,R2 are respectively H, halogen, azido, lower alkyl, or together methylene group; B is pyrimidine of uracil, cytosin, thymine, 5-halouracil, 5-halocytosin etc, or guanine, 6-chloropurine, hypoxanthine, 2-amino-6-cyclopropylamine, 6-methoxypurine, and 2-amino-6-methoxypurine. The acute toxicity test of thionucleosides is conducted with mice. Each compound is crushed and mixed with corn oil to afford 250 mg/kg, 1,000 mg/kg and 2,000 mg/kg. Dosage of 10 ml or 20 ml per kg is administered by using a needle for oral administration. The percentage of mortality is shown 0% to 2,000 mg/kg.
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