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Title: Toward the discovery of novel anti-HIV drugs. Second-generation Inhibitors of the cellular ATPase DDX3 with Improved anti-HIV activity: Synthesis, Structure-activity relationship analysis, cytotoxicity studies, and target validation
Authors: Maga, Giovanni
Falchi, Federico
Radi, Marco
Botta, Lorenzo
Casaluce, Gianni
Bernardini, Martina
Irannejad, Hamid
Manetti, Fabrizio
Garbelli, Anna
Samuele, Alberta
Zanoli, Samantha
Esté, José A
Gonzalez, Emmanuel
Zucca, Elisa
Paolucci, Stefania
Baldanti, Fausto
De Rijck, Jan
Debyser, Zeger
Botta, Maurizio # ×
Issue Date: Jun-2011
Publisher: Wiley - V C H Verlag GmbH & Co. KGaA
Series Title: ChemMedChem vol:6 issue:8 pages:1371-1389
Article number: 10.1002/cmdc.201100166
Abstract: A hit optimization protocol applied to the first nonnucleoside inhibitor of the ATPase activity of human DEAD-box RNA helicase DDX3 led to the design and synthesis of second-generation rhodanine derivatives with better inhibitory activity toward cellular DDX3 and HIV-1 replication. Additional DDX3 inhibitors were identified among triazine compounds. Biological data were rationalized in terms of structure-activity relationships and docking simulations. Antiviral activity and cytotoxicity of selected DDX3 inhibitors are reported and discussed. A thorough analysis confirmed human DDX3 as a valid anti-HIV target. The compounds described herein represent a significant advance in the pursuit of novel drugs that target HIV-1 host cofactors.
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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