Inhibition of the strand transfer step of HIV-1 integrase by non-natural dinucleotides

被引：22
作者：
Chi, GC
Neamati, N
Nair, V [1 ]
机构：
[1] Univ Georgia, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 USA
[2] Univ So Calif, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 19期
关键词：
HIV integrase; dinucleotides; strand transfer inhibitors;
D O I：
10.1016/j.bmcl.2004.07.050
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
New, non-natural dinucleotide 5'-monophosphates, with a surrogate isonucleoside component Of L-related stereochemistry at the 'terminal' position, have been synthesized. Structures of 2a-c were confirmed by multinuclear NMR spectra (H-1, C-13, (31)p, COSY), UV hypochromicity and FAB HRMS data. These compounds are totally resistant to cleavage by 3'- and 5'-exonucleases. The dinucleotides showed remarkable selectivity for inhibition of the strand transfer step of HIV-1 integrase. To the best of our knowledge, these compounds represent only the second example of selective strand transfer inhibitors of HIV integrase. (C) 2004 Elsevier Ltd. All rights reserved.
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收藏
页码：4815 / 4817
页数：3
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