title: Antiretroviral activity of metal-chelating HIV-1 integrase inhibitors.
abstract: 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.
authors.affiliation: Dipartimento di Chimica, Università di Parma, Parco Area delle Scienze 17/A, I-43124 Parma, Italy. Electronic address: mauro.carcelli@unipr.it.
authors.forename: Mauro
authors.initials: M
authors.lastname: Carcelli
authors.affiliation: Dipartimento di Chimica, Università di Parma, Parco Area delle Scienze 17/A, I-43124 Parma, Italy.
authors.forename: Dominga
authors.initials: D
authors.lastname: Rogolino
authors.affiliation: Dipartimento di Chimica e Farmacia, Università di Sassari, Via Vienna 2, I-07100 Sassari, Italy.
authors.forename: Mario
authors.initials: M
authors.lastname: Sechi
authors.affiliation: Dipartimento di Chimica, Università di Parma, Parco Area delle Scienze 17/A, I-43124 Parma, Italy.
authors.forename: Gabriele
authors.initials: G
authors.lastname: Rispoli
authors.affiliation: Dipartimento di Farmacia, Università di Parma, Parco Area delle Scienze 27/A, I-43124 Parma, Italy.
authors.forename: Emilia
authors.initials: E
authors.lastname: Fisicaro
authors.affiliation: Dipartimento di Farmacia, Università di Parma, Parco Area delle Scienze 27/A, I-43124 Parma, Italy.
authors.forename: Carlotta
authors.initials: C
authors.lastname: Compari
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente-Sezione Biomedica-Università di Cagliari Cittadella Universitaria SS554, I-09042 Monserrato, CA, Italy.
authors.forename: Nicole
authors.initials: N
authors.lastname: Grandi
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente-Sezione Biomedica-Università di Cagliari Cittadella Universitaria SS554, I-09042 Monserrato, CA, Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Corona
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente-Sezione Biomedica-Università di Cagliari Cittadella Universitaria SS554, I-09042 Monserrato, CA, Italy.
authors.forename: Enzo
authors.initials: E
authors.lastname: Tramontano
authors.affiliation: Rega Institute for Medical Research, KU Leuven, B-3000 Leuven, Belgium.
authors.forename: Christophe
authors.initials: C
authors.lastname: Pannecouque
authors.affiliation: Rega Institute for Medical Research, KU Leuven, B-3000 Leuven, Belgium.
authors.forename: Lieve
authors.initials: L
authors.lastname: Naesens
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002614:Chelating Agents / Q000737:chemistry / Q000494:pharmacology*; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology*; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D015498:HIV-2 / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008024:Ligands; D013816:Thermodynamics
chemical_list: D019380:Anti-HIV Agents; D002614:Chelating Agents; D056831:Coordination Complexes; D019428:HIV Integrase Inhibitors; D008024:Ligands; D019427:HIV Integrase
keywords: Antiviral agents; Dual inhibitors; HIV-1 RNase H inhibitors; HIV-1 integrase inhibitors; Metal complexes