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- Title
New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses.
- Authors
Rusconi, Stefano; Cicero, Mirko Lo; Viganò, Ottavia; Sirianni, Francesca; Bulgheroni, Elisabetta; Ferramosca, Stefania; Bencini, Andrea; Bianchi, Antonio; Ruiz, Lidia; Cabrera, Cecilia; Martinez-Picado, Javier; Supuran, Claudiu T.; Galli, Massimo
- Abstract
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.
- Subjects
POLYAMINES; ALIPHATIC compounds; ETHYLENEDIAMINE; PROPANEDIAMINE; CHEMOKINES; INFLAMMATORY mediators; PEPTIDES; MACROCYCLIC compounds; CROWN ethers
- Publication
Molecules, 2009, Vol 14, Issue 5, p1927
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules14051927