Title: Synthesis and biological evaluation of novel antiviral agents as protein-protein interaction inhibitors
Authors: Ferro, Stefania
De Luca, Laura
Morreale, Francesca
Christ, Frauke
Debyser, Zeger
Gitto, Rosaria
Chimirri, Alba # ×
Issue Date: Apr-2014
Publisher: Taylor & Francis
Series Title: Journal of Enzyme Inhibition and Medicinal Chemistry vol:29 issue:2 pages:237-242
Abstract: Abstract In continuation of our research efforts toward the identification and optimization for novel inhibitors of interaction between human immunodeficiency virus type 1 integrase and cellular cofactor LEDGF/p75, we designed and synthesized a new series of 4-benzylindole derivatives. Most of the title compounds proved to be able to block this protein-protein interaction (PPI), with a percentage ranging from 30% to 90% at 100 µM. The most promising derivative was compound 10b showing IC50 value of 6.41 µM. The main structure-activity relationships (SAR) are discussed and rationalized by docking studies.
ISSN: 1475-6366
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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