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Molecules 2009, 14(5), 1927-1937; doi:10.3390/molecules14051927

New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses

1,* , 1, 1, 1, 1, 1, 2, 2, 3, 3, 3
1 Dipartimento di Scienze Cliniche “Luigi Sacco”, Sezione di Malattie Infettive e Immunopatologia, Università degli Studi, Ospedale Luigi Sacco, via G.B. Grassi 74, 20157 Milano, Italy 2 Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Firenze), Italy 3 IrsiCaixa Foundation, University Hospital Germans Trias i Pujol, Badalona, Spain
* Author to whom correspondence should be addressed.
Received: 2 April 2009 / Revised: 20 May 2009 / Accepted: 21 May 2009 / Published: 22 May 2009
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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.
Keywords: HIV-1; co-receptors; CXCR4; macrocyclic polyamines HIV-1; co-receptors; CXCR4; macrocyclic polyamines
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Rusconi, S.; Cicero, M.L.; Viganò, O.; Sirianni, F.; Bulgheroni, E.; Ferramosca, S.; Bencini, A.; Bianchi, A.; Ruiz, L.; Cabrera, C.; Martinez-Picado, J.; Supuran, C.T.; Galli, M. New Macrocyclic Amines Showing Activity as HIV Entry Inhibitors Against Wild Type and Multi-Drug Resistant Viruses. Molecules 2009, 14, 1927-1937.

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