| Autor: |
Massimo Galli, Cecilia Cabrera, Javier Martinez-Picado, Claudiu T. Supuran, Lidia Ruiz, Antonio Bianchi, Elisabetta Bulgheroni, Andrea Bencini, Stefania Ferramosca, Ottavia Viganò, Stefano Rusconi, Francesca Sirianni, Mirko Lo Cicero |
| Jazyk: |
angličtina |
| Rok vydání: |
2009 |
| Předmět: |
|
| Zdroj: |
Molecules, Vol 14, Iss 5, Pp 1927-1937 (2009) |
| Druh dokumentu: |
article |
| ISSN: |
1420-3049 |
| DOI: |
10.3390/molecules14051927 |
| Popis: |
Considering as a lead molecule the chemokine CXCR4 receptor antagonist AMD-3100, which shows significant anti-HIV activity in vitro and in vivo, we investigated a series of structurally related macrocyclic polyamines incorporating o,o’-phenanthroline or 2,2’-bipyridyl scaffolds as potential antiviral agents with lower toxicity and increased activity against both wild type X4-tropic and dual tropic HIV strains. The antiviral activity of these compounds was evaluated by susceptibility assays in PBMC (Peripheral Blood Mononuclear Cells) and compared to that of AMD-3100. The newly investigated compounds showed IC50s values in the low micromolar range and significantly inhibited the viral replication of wild type X4-tropic isolate and dual tropic strains. These macrocyclic polyamines constitute a promising class of HIV entry inhibitors. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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