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.

New macrocyclic amines showing activity as HIV entry inhibitors against wild type and multi-drug resistant viruses / S. Rusconi, M. Lo 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. - 14:5(2009 May 22), pp. 1927-1937.

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

S. Rusconi
Primo
;
M. Lo Cicero
Secondo
;
O. Viganò;S. Ferramosca;M. Galli
Ultimo
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 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.
HIV-1 ; co-receptors ; CXCR4 ; macrocyclic polyamines;
Settore MED/17 - Malattie Infettive
22-mag-2009
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/65551
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