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 IC(50)s 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.

New macrocyclic amines showing activity as HIV entry inhibitors against wild type and multi-drug resistant viruses / S. Rusconi;M. L. Cicero;O. Viganò;F. Sirianni;E. Bulgheroni;S. Ferramosca;A. Bencini;A. Bianchi;L. Ruiz;C. Cabrera;J. Martinez-Picado;C. T. Supuran;M. Galli. - In: MOLECULES. - ISSN 1420-3049. - STAMPA. - 14:(2009), pp. 1927-1937. [10.3390/molecules14051927]

New macrocyclic amines showing activity as HIV entry inhibitors against wild type and multi-drug resistant viruses.

BENCINI, ANDREA;BIANCHI, ANTONIO;SUPURAN, CLAUDIU TRANDAFIR;
2009

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 IC(50)s 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.
2009
14
1927
1937
S. Rusconi;M. L. Cicero;O. Viganò;F. Sirianni;E. Bulgheroni;S. Ferramosca;A. Bencini;A. Bianchi;L. Ruiz;C. Cabrera;J. Martinez-Picado;C. T....espandi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/776163
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