Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5933
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, G
Falchi, F
Botta, Maurizio 
Botta, L
Casaluce, G
Bernardini, M
Irannejad, H
Manetti, Fabrizio 
Garbelli, A
Samuele, A
Zanoli, S
ESTÈ J., A
Gonzales, E
Zucca, E
Paolucci, S
Baldanti, F
DE RIJCK, J
Debyser, Z
Botta, Maurizio 
Keywords: Antiviral agents; DDX3, Helicase; HIV-1; Host cofactors; Inhibitors
Issue Date: 2011
Project: None 
Journal: CHEMMEDCHEM
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.
Description: 
25298
URI: http://hdl.handle.net/20.500.12779/5933
ISSN: 1860-7179
DOI: 10.1002/cmdc.201100166
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