Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue -, Pages 361-369Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.02.015
Keywords
Raltegravir derivatives; Anti-HIV activity; Subpicomole IC50 value; 5-Hydroxyl modification; High-throughput cell-based assay method; Pseudotyped virus stocks
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Funding
- Chinese Ministry of Health [2008ZX 10001-002]
- China Postdoctoral Science Foundation [2011M500519]
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A series of raltegravir derivatives 20-42 were prepared and systematically evaluated for their anti-HIV activity. The bioassay results showed that most of the compounds possess good to excellent anti-HIV activity. Especially, compounds 25 and 35 with subpicomole IC50 values seemed to be the most potent anti-HIV agents among all of the reported synthesized compounds. These compounds may therefore be considered as new potent anti-HIV agents. The 5-hydroxyl modification of raltegravir derivatives significantly increased the anti-HIV activity, which indicates that the hydroxyl may not be indispensable for raltegravir. The introducing of acyl at 5-position of raltegravir derivatives is favorable for antiviral activity. In addition, a high-throughput cell-based assay method with pseudotyped virus stocks was developed and used to identify HIV inhibitors. (C) 2012 Elsevier Masson SAS. All rights reserved.
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