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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, G
ESTÈ J., A
DE RIJCK, J
|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.
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