Effect of the extent of thiolation and introduction of phosphorothioate internucleotide linkages on the anti-HIV activity of Suligovir [(s⁴dU)₃₅]

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• 作者：Andrá ; s Horvá ; th ; Zoltá ; n Beck ; Thomas J. Bardos ; Joseph A. Dunn and Janos Aradi
• 关键词：Chemically modified oligonucleotides ; 4-Thio-oligo-deoxyuridylate ; Suligovir ; HIV ; HIV entry ; Anti-HIV
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 October 2006
• 年：2006
• 卷：16
• 期：20
• 页码：5321-5323
• 全文大小：121 K

文摘

Suligovir is a 35-mer homo-oligonucleotide, containing exclusively 4-thio deoxyuridylate, proved to be a potent inhibitor of HIV entry. In this paper, we described the effect of extent of thiolation and the introduction of nuclease-resistant phosphorothioate linkages on the anti-HIV activity of Suligovir. We found that the decreased thiolated nucleotide content decreases the anti-HIV potency of the compound and the introduction of phosphorothioate linkages does not improve its antiviral activity.