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Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Apr 01; Vol. 25 (7), pp. 1568-71. Date of Electronic Publication: 2015 Feb 16. - Publication Year :
- 2015
-
Abstract
- Twenty-four derivatives of erythrocentaurin (ET) were synthesized and evaluated for their anti-HBV activities on HepG 2.2.15 cell line in vitro. Eight compounds 1, 2, 5, 8, 9, 1e, 1k, and 1m increased activity against HBV DNA replication with the SI values higher than 11. In particular, derivatives 1e and 1k exhibited the most potent inhibition on HBV DNA replication with the IC50 values of 0.026 mM (SI>70.8) and 0.045 mM (SI>36.0), respectively. The primary structure-activity relationships (SARs) of ET derivatives were summarized for exploring potent anti-HBV agents.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antiviral Agents chemical synthesis
Antiviral Agents chemistry
Dose-Response Relationship, Drug
Hep G2 Cells
Humans
Isocoumarins chemical synthesis
Isocoumarins chemistry
Microbial Sensitivity Tests
Molecular Structure
Antiviral Agents pharmacology
Hepatitis B virus drug effects
Isocoumarins pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 25737009
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.02.009