Synthesis and anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives

被引：103
作者：
Bosi, S
Da Ros, T
Spalluto, G
Balzarini, J
Prato, M
机构：
[1] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium
[2] Univ Trieste, Dipartimento Sci Farmaceut, I-34127 Trieste, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 24期
关键词：
D O I：
10.1016/j.bmcl.2003.09.016
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of bis-functionalized fullerene C(60) derivatives bearing two or more solubilizing chains have been evaluated for their activity against HIV-1 and HIV-2 strains. Some of the compounds show activity against HIV-1 type in the low micromolar range. The effect of the positions of the addends on the C(60) nucleus has been investigated, indicating that only trans-2 isomers possess promising activity. The presence of a quaternary pyrrolidinium nitrogen is essential to increase solubility. (C) 2003 Elsevier Ltd. All rights reserved.
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页码：4437 / 4440
页数：4
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