期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 10, 页码 3354-3365出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801608u
关键词
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资金
- MIUR (PRIN 2006, Roma, Italy)
- Fonds voor Wetenschappelijk Onderzoek Vlaanderen
- Fondazione Buzzati-Traverso Fellowship
We report the synthesis and structure - activity relationship (SAR) of a large series of acridones and acridone-fragment derivatives designed on the basis of the selective antihepatitis C virus (HCV) activity shown by acridone 2, previously studied as a potential antibovine viral diarrhea virus (BVDV) compound. The evaluation of their ability to inhibit the HCV replication in Huh-5-2 cells led to the identification of new, selective inhibitors. This indicates that the acridone skeleton, when properly functionalized, is a suitable scaffold to obtain potential anti-HCV agents. Interestingly, during identification of possible cellular and viral targets, it was discovered that compound 23 exerts inhibitory activity on the HCV NS3 helicase, a very promising target for the development of anti-HCV drugs.
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