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Title: A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series
Authors: De Luca, Laura
Barreca, Maria Letizia
Ferro, Stefania
Iraci, Nunzio
Michiels, Martine
Christ, Frauke
Debyser, Zeger
Witvrouw, Myriam
Chimirri, Alba # ×
Issue Date: May-2008
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:18 issue:9 pages:2891-2895
Abstract: We report herein the development of a new three-dimensional pharmacophore model for HIV-1 integrase inhibitors which led to the discovery of some 4-[1-(4-fluorobenzyl)-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acids that are able to specifically inhibit the strand transfer step of integration at nanomolar concentration. The synthesis of the new designed molecules is also described. (c) 2008 Elsevier Ltd. All rights reserved.
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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