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Antiretroviral activity of metal-chelating HIV-1 integrase inhibitors

Carcelli, Mauro and Rogolino, Dominga and Sechi, Mario and Rispoli, Gabriele and Fisicaro, Emilia and Compari, Carlotta and Grandi, Nicole and Corona, Angela and Tramontano, Enzo and Pannecouque, Christophe and Naesens, Lieve (2014) Antiretroviral activity of metal-chelating HIV-1 integrase inhibitors. European Journal of Medicinal Chemistry, Vol. 83 , p. 594-600. ISSN 0223-5234. Article.

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DOI: 10.1016/j.ejmech.2014.06.055


Data regarding the activity of metal complexes against HIV virus in cell are surprisingly scarce. In this study, we present the antiviral activity against HIV-infected cells of different types of chelating ligands and of their metal complexes. In particular, the carboxamide chelating scaffold and the corresponding coordination compounds demonstrated an interesting antiviral profile in the nanomolar range. These molecules inhibit not only HIV integrase catalytic activity, but they also interfere with the function of the RNase H component of the HIV reverse transcriptase. Here we also discuss the thermodynamic characterization in solution of the metal complexes of the most active ligands, affording to the best of our knowledge for the first time this type of data for complexes with anti-HIV activity.

Item Type:Article
ID Code:10002
Uncontrolled Keywords:Antiviral agents, HIV-1 integrase inhibitors, HIV-1 RNase H inhibitors, metal complexes, dual inhibitors
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier Masson
Deposited On:06 Aug 2014 13:53

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