Journal
CHEMMEDCHEM
Volume 6, Issue 8, Pages 1371-1389Publisher
WILEY-BLACKWELL
DOI: 10.1002/cmdc.201100166
Keywords
antiviral agents; DDX3; helicase; HIV-1; host cofactors; inhibitors
Categories
Funding
- 6th FP Excellent-Hit Consortium [LSHP-CT-2006-037257]
- Italian National Program of AIDS Research [40H26]
- European Union [HEALTH-2007-2.3.2-1, HEALTH-F3-2009-242135]
- Italian Ministero dell'Istruzione, dell'Universita e della Ricerca [2008CE75SA 004]
- Franca Rame and Dario Fo Nobel Foundation
- Ministero della Sanita
- Fondazione IRCCS Policlinico San Matteo
- Ricerca Corrente [80622]
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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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