Abstract |
From random screening of our compound libraries, we identified a hit compound with an IC50 of 27 microM against hepatitis C viral NS5B RNA-dependent RNA polymerase. By using a parallel synthetic strategy, a series of its derivatives were synthesized. From their anti-HCV activity screening, compounds with single digital 3.8 micromolar activity were obtained.
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Authors | Yili Ding, Jean-Luc Girardet, Kenneth L Smith, Gary Larson, Brett Prigaro, Jim Z Wu, Nanhua Yao |
Journal | Bioorganic chemistry
(Bioorg Chem)
Vol. 34
Issue 1
Pg. 26-38
(Feb 2006)
ISSN: 0045-2068 [Print] United States |
PMID | 16360193
(Publication Type: Journal Article)
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Chemical References |
- 2-Pyridin-2-yl-1H-indole
- Antiviral Agents
- Enzyme Inhibitors
- Indoles
- Pyridines
- Viral Nonstructural Proteins
- 5-cyanouracil
- Uracil
- NS-5 protein, hepatitis C virus
- RNA-Dependent RNA Polymerase
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Topics |
- Antiviral Agents
(chemical synthesis, pharmacology)
- Enzyme Inhibitors
(chemical synthesis, pharmacology)
- Hepacivirus
(drug effects, enzymology)
- Humans
- Indoles
(chemical synthesis, metabolism)
- Inhibitory Concentration 50
- Pyridines
(chemical synthesis, metabolism)
- RNA-Dependent RNA Polymerase
(antagonists & inhibitors, metabolism)
- Structure-Activity Relationship
- Uracil
(analogs & derivatives, chemical synthesis, pharmacology)
- Viral Nonstructural Proteins
(genetics, metabolism)
- Virus Replication
(drug effects)
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