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Title: New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action
Authors: Ferro, Stefania
De Luca, Laura ×
Barreca, Maria Letizia
De Grazia, Sara
Christ, Frauke
Debyser, Zeger
Chimirri, Alba #
Issue Date: Aug-2010
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:18 issue:15 pages:5510-5518
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.
URI: 
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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