L-异核苷掺入的二核苷酸的合成与抗HIV活性研究

doi:10.5246/jcps.2013.04.045

L-异核苷掺入的二核苷酸的合成与抗HIV活性研究

王萌, 邢磊, 陆世芳, 关注^*, 杨振军, 张礼和

北京大学医学部天然药物及仿生药物国家重点实验室; 药学院药物化学系, 北京 100191

收稿日期:2013-03-25 修回日期:2013-04-11 出版日期:2013-07-10 发布日期:2013-07-10
通讯作者: 关注*

Synthesis and the anti-HIV activity of novel dinucleotides containing
L-isonucleosides

Meng Wang, Lei Xing, Shifang Lu, Zhu Guan^*, Zhenjun Yang, Lihe Zhang

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, Chin

Received:2013-03-25 Revised:2013-04-11 Online:2013-07-10 Published:2013-07-10
Contact: Zhu Guan*

摘要/Abstract

摘要：

本论文利用亚磷酰胺一釜法合成了三个5'-端L-构型异核苷掺入的非天然二核苷酸, 对它们与HIV整合酶的结合模式进行了模拟, 并对它们在假病毒体系中的抗HIV活性进行了评价。

关键词: HIV整合酶, 二核苷酸, 合成, 抗-HIV, 结合模式

Abstract: Three dinucleotides containing L-isonucleosides at 5'-end were synthesized by an elegant phosphoramidite one-pot method. Their binding modes with HIV integrase were simulated and their anti-HIV activities in pseudotyped virus system were examined.

Key words: HIV integrase, Dinucleotides, Synthesis, Anti-HIV, Binding modes

中图分类号:

R916

Supporting: Foundation items: National Natural Science Foundation of China (Grant No. 20832008 and 21002004).
^*Corresponding author. Tel./Fax: 86-10-82805023

王萌, 邢磊, 陆世芳, 关注^*, 杨振军, 张礼和. L-异核苷掺入的二核苷酸的合成与抗HIV活性研究[J]. , DOI: 10.5246/jcps.2013.04.045.

Meng Wang, Lei Xing, Shifang Lu, Zhu Guan^*, Zhenjun Yang, Lihe Zhang. Synthesis and the anti-HIV activity of novel dinucleotides containing
L-isonucleosides[J]. , DOI: 10.5246/jcps.2013.04.045.

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