期刊
JOURNAL OF BIOMOLECULAR SCREENING
卷 13, 期 9, 页码 879-887出版社
SAGE PUBLICATIONS INC
DOI: 10.1177/1087057108323123
关键词
influenza; HTS; high-throughput screening; antivirals
资金
- National Institutes of Health [N01-AI-30047]
Using a highly reproducible and robust cell-based high-throughput screening (HTS) assay, the authors screened a 100,000-compound library at 14- and 114-mu M compound concentration against influenza strain A/Udorn/72 (H3N2). The hit rates (>50% inhibition of the viral cytopathic effect) from the 14- and 114-mu M screens were 0.022% and 0.38%, respectively. The hits were evaluated for their antiviral activity, cell toxicity, and selectivity in dose-response experiments. The screen at the lower concentration yielded 3 compounds, which displayed moderate activity (SI50 = 10-49). Intriguingly, the screen at the higher concentration revealed several additional hits. Two of these hits were highly active with an SI50 > 50. Time of addition experiments revealed 1 compound that inhibited early and 4 other compounds that inhibited late in the virus life cycle, suggesting they affect entry and replication, respectively. The active compounds represent several different classes of molecules such as carboxanilides, 1-benzoyl-3-arylthioureas, sulfonamides, and benzothiazinones, which have not been previously identified as having antiviral/anti-influenza activity. (Journal of Biomolecular Screening 2008:879-887)
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