寡脱氧核糖核苷酸的硫代磷酸酯类似物：合成及其作为人类免疫缺陷病毒复制抑制剂的活性
Phosphorothioate analogues of oligodeoxyribonucleotide: synthesis and activity as inhibitors of replication of human immunodeficiency virus.
作者信息
Kim S G, Suzuki Y, Nakashima H, Yamamoto N, Takaku H
机构信息
Department of Industrial Chemistry, Chiba Institute of Technology, Japan.
出版信息
Biochem Biophys Res Commun. 1991 Sep 30;179(3):1614-9. doi: 10.1016/0006-291x(91)91759-6.
The modifications of oligodeoxyribonucleotides include replacement of the other chain either all-PS (S-ODNs), or end-capped with several PS (SO-ODNs) groups at both 3'- and 5'-ends. A general synthesis of phosphorothioate analogues of oligodeoxyribonucleotides is described using the new phosphite. In assays of HIV, oligomers (S-ODNs) with complete replacement of phosphodiesters with phosphorothioate groups were found to be very active. Finally of particular interest is S-ODNs-rev or tat (20mers) which possessed slightly higher anti-HIV activity than S-dC28 itself. By contrast, the unmodified oligomers (ODNs) as well as SO-ODNs did not have any inhibitory effect.
寡脱氧核糖核苷酸的修饰包括用全硫代磷酸酯（S-ODNs）替换另一条链，或在3'和5'末端均用几个硫代磷酸酯（SO-ODNs）基团进行封端。使用新型亚磷酸酯描述了寡脱氧核糖核苷酸硫代磷酸酯类似物的一般合成方法。在HIV检测中，发现磷酸二酯完全被硫代磷酸酯基团取代的寡聚物（S-ODNs）具有很高的活性。最后，特别值得关注的是S-ODNs-rev或tat（20聚体），其抗HIV活性略高于S-dC28本身。相比之下，未修饰的寡聚物（ODNs）以及SO-ODNs没有任何抑制作用。
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