2'-脱氧-5-乙烯基尿苷和2'-脱氧-5-乙烯基胞苷的合成及生物学特性
Synthesis and biological properties of 2'-deoxy-5-vinyluridine and 2'deoxy-5-vinylcytidine.
作者信息
Rahim S G, Duggan M J, Walker R T, Jones A S, Dyer R L, Balzarini J, De Clercq E
出版信息
Nucleic Acids Res. 1982 Sep 11;10(17):5285-95. doi: 10.1093/nar/10.17.5285.
Abstract
Rapid and efficient syntheses for the preparation of 2'-deoxy-5-vinyluridine and 2'-deoxy-5-vinylcytidine are described starting from nucleoside precursors. Contrary to some previous reports, 2-deoxy-5-vinyluridine has be found to be quite stable under normal laboratory conditions but when tested in animals shows neither toxicity nor anti-leukemic (L1210 cells) or anti-parasitic (Plasmodium berghei) activity. 2'-Deoxy-5-vinylcytidine appears to polymerise readily. It is much less toxic to cell cultures than 2'-deoxy-5'vinyluridine but is almost as active against herpes virus replication (ID50:0.2 microgram/ml) for both type 1 and type 2 herpes virus (selectivity index:225).
摘要
描述了从核苷前体开始快速高效合成2'-脱氧-5-乙烯基尿苷和2'-脱氧-5-乙烯基胞苷的方法。与之前的一些报道相反，已发现2-脱氧-5-乙烯基尿苷在正常实验室条件下相当稳定，但在动物试验中既无毒性，也没有抗白血病（L1210细胞）或抗寄生虫（伯氏疟原虫）活性。2'-脱氧-5-乙烯基胞苷似乎很容易聚合。它对细胞培养物的毒性比2'-脱氧-5'-乙烯基尿苷小得多，但对1型和2型疱疹病毒的疱疹病毒复制几乎具有相同的活性（半数抑制浓度：0.2微克/毫升）（选择性指数：225）。
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