New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action |
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| Authors: | Stefania Ferro Laura De Luca Maria Letizia Barreca Sara De Grazia Frauke Christ Zeger Debyser Alba Chimirri |
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| Institution: | 1. Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, I-98168 Messina, Italy;2. Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo, 1, I-06123 Perugia, Italy;3. Molecular Virology and Gene Therapy, Molecular Medicine, Katholieke Universiteit Leuven and IRC KULAK, Kapucijnenvoer 33, B-3000 Leuven, Flanders, Belgium |
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| Abstract: | The life cycle of HIV-1 requires extensive assistance from the integrase (IN) enzyme which therefore constitutes an attractive therapeutic target for the development of anti-AIDS agents. We herein report the synthesis and biological evaluation of new HIV integrase strand-transfer inhibitors (INSTIs) which proved to be also potent anti-HIV agents. The binding mode of the most representative molecules were also studied by induced-fit docking (IFD). The obtained IFD results were consistent with the mechanism of action proposed for this class of IN inhibitors, that is metal chelating/binding agents. |
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