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Title: Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity
Authors: Suchaud, Virginie
Bailly, Fabrice ×
Lion, Cédric
Tramontano, Enzo
Esposito, Francesca
Corona, Angela
Christ, Frauke
Debyser, Zeger
Cotelle, Philippe #
Issue Date: Jun-2012
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:22 issue:12 pages:3988-3992
Abstract: We report herein the synthesis of a series of 3-hydroxyquinolin-2(1H)-one derivatives. Esters and amide groups were introduced at position 4 of the basis scaffold and some modulations of the benzenic moiety were performed. Most compounds presented selective inhibitory properties in the 10-20μM range against HIV-1 reverse transcriptase associated ribonuclease H activity, without affecting the integrase and reverse transcriptase DNA polymerase activities. Unfortunately all tested compounds exhibited high cellular cytotoxicity in cell culture which limited their applications as antiviral agents.
URI: 
ISSN: 0960-894X
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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