Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors.
Identifieur interne : 000E48 ( PubMed/Corpus ); précédent : 000E47; suivant : 000E49Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors.
Auteurs : Chang-An Geng ; Xiao-Yan Huang ; Yun-Bao Ma ; Xue-Mei Zhang ; Ji-Jun ChenSource :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2015.
English descriptors
- KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Dose-Response Relationship, Drug, Hep G2 Cells, Hepatitis B virus (drug effects), Humans, Isocoumarins (chemical synthesis), Isocoumarins (chemistry), Isocoumarins (pharmacology), Microbial Sensitivity Tests, Molecular Structure.
- MESH :
- chemical , chemical synthesis : Antiviral Agents, Isocoumarins.
- chemical , chemistry : Antiviral Agents, Isocoumarins.
- chemical , pharmacology : Antiviral Agents, Isocoumarins.
- drug effects : Hepatitis B virus.
- Dose-Response Relationship, Drug, Hep G2 Cells, Humans, Microbial Sensitivity Tests, Molecular Structure.
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.
DOI: 10.1016/j.bmcl.2015.02.009
PubMed: 25737009
Links to Exploration step
pubmed:25737009Le document en format XML
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<author><name sortKey="Huang, Xiao Yan" sort="Huang, Xiao Yan" uniqKey="Huang X" first="Xiao-Yan" last="Huang">Xiao-Yan Huang</name>
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<front><div type="abstract" xml:lang="en">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.</div>
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<Abstract><AbstractText>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.</AbstractText>
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