Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors
| Autor: | Zengquan Wei, Wenzhao Liu, Dong Chen, Ping Gong, Yajing Liu, Yanfang Zhao |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
DNA Replication
Hepatitis B virus Stereochemistry Clinical Biochemistry Pharmaceutical Science medicine.disease_cause Antiviral Agents Biochemistry Chemical synthesis Virus Structure-Activity Relationship Cell Line Tumor Drug Discovery medicine Humans Structure–activity relationship Cytotoxicity Molecular Biology Chemistry Organic Chemistry Lamivudine Biological activity In vitro Molecular Medicine Benzimidazoles medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:7230-7233 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.10.099 |
| Popis: | A new series of 1-methyl-1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. Some of the analogues in this series displayed inhibitory activity superior to lamivudine. Of them, compound 13b was the most potent one, showing an IC(50) value of 7.8 μM and a SI value of 13.0. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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