Title: A versatile and practical synthesis toward the development of novel HIV-1 integrase inhibitors
Authors: Rinaldi, Marta
Tintori, Cristina
Franchi, Luigi
Vignaroli, Giulia
Innitzer, Anna
Massa, Silvio
Esté, José A
Gonzalo, Encarna
Christ, Frauke
Debyser, Zeger
Botta, Maurizio # ×
Issue Date: Jan-2011
Publisher: Wiley - V C H Verlag GmbH & Co. KGaA
Series Title: ChemMedChem vol:6 issue:2 pages:343-352
Article number: 10.1002/cmdc.201000510
Abstract: As a continuation of our previous work, which resulted in the identification of a new hit compound as an HIV-1 integrase inhibitor, three novel series of salicylic acid derivatives were synthesized using three versatile and practical synthetic strategies and were assayed for their capacity to inhibit the catalytic activity of HIV-1 integrase. Biological evaluations revealed that some of the synthesized compounds possess good inhibitory potency in enzymatic assays and are able to inhibit viral replication in MT-4 cells at low micromolar concentrations. Finally, docking studies were conducted to analyze the binding mode of the synthesized compounds within the DNA binding site of integrase in order to refine their structure-activity relationships.
ISSN: 1860-7179
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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