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Synthesis and anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives |
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| Authors: | Bosi Susanna Da Ros Tatiana Spalluto Giampiero Balzarini Jan Prato Maurizio |
| Affiliation: | a Dipartimento di Scienze Farmaceutiche, Università di Trieste, Piazzale Europa 1, I-34127, Trieste, Italy b Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Minderbroedersstraat 10, B-3000, Leuven, Belgium |
| 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-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 C60 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. |
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