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

Abstract—A new series of bis-functionalized fullerene C60 derivatives bearing two or more solubilizing chains have been evaluated for their activity against HIV-1 and HIV-2strains. 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 C60 nucleus has been investigated, indicating that only trans-2isomers possess promising activity. The presence of a quaternary pyrrolidinium nitrogen is essential to increase solubility.



Titolo: Synthesis and anti-HIV properties of new water-soluble bis-functionalized [60]fullerene derivatives
Autori: 
BOSI, Susanna
DA ROS, TATIANA
SPALLUTO, GIAMPIERO
PRATO, MAURIZIO
mostra contributor esterni 
Data di pubblicazione: 2003
Rivista: 
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS  
Abstract: Abstract—A new series of bis-functionalized fullerene C60 derivatives bearing two or more solubilizing chains have been evaluated for their activity against HIV-1 and HIV-2strains. 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 C60 nucleus has been investigated, indicating that only trans-2isomers possess promising activity. The presence of a quaternary pyrrolidinium nitrogen is essential to increase solubility.
Handle: http://hdl.handle.net/11368/1693534
Appare nelle tipologie:1.1 Articolo in Rivista

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