New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action

Bioorganic & Medicinal Chemistry
Stefania FerroAlba Chimirri

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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Citations

Sep 26, 2012·Expert Opinion on Drug Discovery·Sara SadlerGraham B Jones
Apr 1, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Stefania FerroRosaria Gitto
Jan 14, 2011·European Journal of Medicinal Chemistry·Laura De LucaAlba Chimirri
Jul 19, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Laura De LucaRosaria Gitto

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