Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors.
Identifieur interne : 001230 ( Main/Exploration ); précédent : 001229; suivant : 001231Synthesis of erythrocentaurin derivatives as a new class of hepatitis B virus inhibitors.
Auteurs : Chang-An Geng [République populaire de Chine] ; Xiao-Yan Huang [République populaire de Chine] ; Yun-Bao Ma [République populaire de Chine] ; Xue-Mei Zhang [République populaire de Chine] ; Ji-Jun Chen [République populaire de Chine]Source :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2015.
Descripteurs français
- KwdFr :
- Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Cellules HepG2, Humains, Isocoumarines (), Isocoumarines (pharmacologie), Isocoumarines (synthèse chimique), Relation dose-effet des médicaments, Structure moléculaire, Tests de sensibilité microbienne, Virus de l'hépatite B ().
- MESH :
- pharmacologie : Antiviraux, Isocoumarines.
- synthèse chimique : Antiviraux, Isocoumarines.
- Antiviraux, Cellules HepG2, Humains, Isocoumarines, Relation dose-effet des médicaments, Structure moléculaire, Tests de sensibilité microbienne, Virus de l'hépatite B.
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
Affiliations:
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Electronic address: chenjj@mail.kib.ac.cn.</nlm:affiliation><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201</wicri:regionArea><wicri:noRegion>Kunming 650201</wicri:noRegion></affiliation></author></analytic><series><title level="j">Bioorganic & medicinal chemistry letters</title><idno type="eISSN">1464-3405</idno><imprint><date when="2015" type="published">2015</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral Agents (chemical synthesis)</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (pharmacology)</term><term>Dose-Response Relationship, Drug</term><term>Hep G2 Cells</term><term>Hepatitis B virus (drug effects)</term><term>Humans</term><term>Isocoumarins (chemical synthesis)</term><term>Isocoumarins (chemistry)</term><term>Isocoumarins (pharmacology)</term><term>Microbial Sensitivity Tests</term><term>Molecular Structure</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Antiviraux ()</term><term>Antiviraux (pharmacologie)</term><term>Antiviraux (synthèse chimique)</term><term>Cellules HepG2</term><term>Humains</term><term>Isocoumarines ()</term><term>Isocoumarines (pharmacologie)</term><term>Isocoumarines (synthèse chimique)</term><term>Relation dose-effet des médicaments</term><term>Structure moléculaire</term><term>Tests de sensibilité microbienne</term><term>Virus de l'hépatite B ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antiviral Agents</term><term>Isocoumarins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antiviral Agents</term><term>Isocoumarins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term><term>Isocoumarins</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Hepatitis B virus</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term><term>Isocoumarines</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antiviraux</term><term>Isocoumarines</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Dose-Response Relationship, Drug</term><term>Hep G2 Cells</term><term>Humans</term><term>Microbial Sensitivity Tests</term><term>Molecular Structure</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Antiviraux</term><term>Cellules HepG2</term><term>Humains</term><term>Isocoumarines</term><term>Relation dose-effet des médicaments</term><term>Structure moléculaire</term><term>Tests de sensibilité microbienne</term><term>Virus de l'hépatite B</term></keywords></textClass></profileDesc></teiHeader><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></front></TEI><affiliations><list><country><li>République populaire de Chine</li></country></list><tree><country name="République populaire de Chine"><noRegion><name sortKey="Geng, Chang An" sort="Geng, Chang An" uniqKey="Geng C" first="Chang-An" last="Geng">Chang-An Geng</name></noRegion><name sortKey="Chen, Ji Jun" sort="Chen, Ji Jun" uniqKey="Chen J" first="Ji-Jun" last="Chen">Ji-Jun Chen</name><name sortKey="Huang, Xiao Yan" sort="Huang, Xiao Yan" uniqKey="Huang X" first="Xiao-Yan" last="Huang">Xiao-Yan Huang</name><name sortKey="Ma, Yun Bao" sort="Ma, Yun Bao" uniqKey="Ma Y" first="Yun-Bao" last="Ma">Yun-Bao Ma</name><name sortKey="Zhang, Xue Mei" sort="Zhang, Xue Mei" uniqKey="Zhang X" first="Xue-Mei" last="Zhang">Xue-Mei Zhang</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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