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

被引：102

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.

引用

页码：4437 / 4440

页数：4

共 19 条

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