Synthesis and anti-HIV-1 integrase activity of modified dinucleotides

被引：5

作者：

Aubert, Yves ^{[1
,2
]}

Chassignol, Marcel ^{[1
,2
]}

Roig, Victoria ^{[1
,2
]}

Mbemba, Gladys ^{[3
]}

Weiss, Julien ^{[1
,2
]}

Meudal, Herve ^{[1
,2
]}

Mouscadet, Jean-Francois ^{[3
]}

Asseline, Ulysse ^{[1
,2
]}

机构：

[1] Univ Orleans, CNRS, UPR 4301, Ctr Biophys Mol, F-45071 Orleans 02, France

[2] INSERM, CNRS, UPR 4301, Ctr Biophys Mol, F-45071 Orleans 02, France

[3] ENS Cachan, CNRS, UMR 8113, LBPA, F-94235 Cachan, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 12期

关键词：

HIV-1 integrase inhibitors; Modified dinucleotides; Intercalator-dinucleotide conjugates; VIRUS TYPE-1 INTEGRASE; HIV-1; INTEGRASE; BINDING-PROPERTIES; IN-VITRO; INHIBITORS; OLIGO-2'-DEOXYRIBONUCLEOTIDES; OLIGODEOXYRIBONUCLEOTIDES; RALTEGRAVIR; RESISTANCE; MUTATIONS;

D O I：

10.1016/j.ejmech.2009.09.007

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The synthesis of a series of thirty-eight new modified dinucleotides and dinucleotide conjugate analogues of d-(5')ApC(3') is described. The inhibitory activity of these compounds toward HIV-1 integrase was examined in enzymatic assays using the natural dinucleotide as a reference. Among the compounds, a perylene-dinucleotide conjugate has shown a two micromolar anti-integrase activity due to the presence of both the intercalator and the dinucleotide. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：5029 / 5044

页数：16

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