1279692-45-3Relevant academic research and scientific papers
COMPOUNDS WITH DDX3 INHIBITORY ACTIVITY AND USES THEREOF
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Page/Page column 144-145, (2011/04/25)
The present invention relates to the medical use of the compound of formula 1,2,3 or 4
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
Maga, Giovanni,Falchi, Federico,Radi, Marco,Botta, Lorenzo,Casaluce, Gianni,Bernardini, Martina,Irannejad, Hamid,Manetti, Fabrizio,Garbelli, Anna,Samuele, Alberta,Zanoli, Samantha,Este, Jose A.,Gonzalez, Emmanuel,Zucca, Elisa,Paolucci, Stefania,Baldanti, Fausto,DeRijck, Jan,Debyser, Zeger,Botta, Maurizio
experimental part, p. 1371 - 1389 (2012/07/28)
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.
