1279692-29-3Relevant academic research and scientific papers
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
, 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.
COMPOUNDS WITH DDX3 INHIBITORY ACTIVITY AND USES THEREOF
-
Page/Page column 153, (2011/04/25)
The present invention relates to the medical use of the compound of formula 1,2,3 or 4
