Design, synthesis and biological evaluation of caudatin analogs as potent hepatitis B virus inhibitors.
Identifieur interne : 001337 ( Main/Exploration ); précédent : 001336; suivant : 001338Design, synthesis and biological evaluation of caudatin analogs as potent hepatitis B virus inhibitors.
Auteurs : Li-Jun Wang ; Hao Chen ; Yun-Bao Ma ; Xiao-Yan Huang ; Chang-An Geng ; Xue-Mei Zhang ; Ji-Jun Chen [République populaire de Chine]Source :
- Medicinal chemistry (Shariqah (United Arab Emirates)) [ 1875-6638 ] ; 2015.
Descripteurs français
- KwdFr :
- ADN viral (biosynthèse), Antigènes de surface du virus de l'hépatite B (métabolisme), Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Cellules HepG2, Conception de médicament, Humains, Hétérosides (), Hétérosides (pharmacologie), Hétérosides (synthèse chimique), Relation structure-activité, Réplication de l'ADN (), Structure moléculaire, Stéroïdes (), Stéroïdes (pharmacologie), Stéroïdes (synthèse chimique), Survie cellulaire (), Virus de l'hépatite B (), Virus de l'hépatite B (croissance et développement), Virus de l'hépatite B (génétique).
- MESH :
- biosynthèse : ADN viral.
- croissance et développement : Virus de l'hépatite B.
- génétique : Virus de l'hépatite B.
- métabolisme : Antigènes de surface du virus de l'hépatite B.
- pharmacologie : Antiviraux, Hétérosides, Stéroïdes.
- synthèse chimique : Antiviraux, Hétérosides, Stéroïdes.
- Antiviraux, Cellules HepG2, Conception de médicament, Humains, Hétérosides, Relation structure-activité, Réplication de l'ADN, Structure moléculaire, Stéroïdes, Survie cellulaire, Virus de l'hépatite B.
English descriptors
- KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Cell Survival (drug effects), DNA Replication (drug effects), DNA, Viral (biosynthesis), Drug Design, Glycosides (chemical synthesis), Glycosides (chemistry), Glycosides (pharmacology), Hep G2 Cells, Hepatitis B Surface Antigens (metabolism), Hepatitis B virus (drug effects), Hepatitis B virus (genetics), Hepatitis B virus (growth & development), Humans, Molecular Structure, Steroids (chemical synthesis), Steroids (chemistry), Steroids (pharmacology), Structure-Activity Relationship.
- MESH :
- chemical , biosynthesis : DNA, Viral.
- chemical , chemical synthesis : Antiviral Agents, Glycosides, Steroids.
- chemical , chemistry : Antiviral Agents, Glycosides, Steroids.
- chemical , metabolism : Hepatitis B Surface Antigens.
- chemical , pharmacology : Antiviral Agents, Glycosides, Steroids.
- drug effects : Cell Survival, DNA Replication, Hepatitis B virus.
- genetics : Hepatitis B virus.
- growth & development : Hepatitis B virus.
- Drug Design, Hep G2 Cells, Humans, Molecular Structure, Structure-Activity Relationship.
Abstract
Thirty-nine caudatin analogs were designed and synthesized. Their anti-hepatitis B virus (HBV) activities were evaluated in vitro. Among them, twenty-three compounds showed much better anti-HBV activity than caudatin, and eleven compounds significantly inhibited the HBV DNA replication with IC50 values < 10 μM. Interestingly, three compounds (22, 28, 29) exhibited excellent activity against the secretion of HBsAg (IC50 = 63.02 μM, 52.81 μM, 56.08 μM), HBeAg (IC50 = 204.80 μM, 173.51 μM, 70.39 μM), along with HBV DNA replication (IC50 = 24.55 μM, 5.69 μM, 8.23 μM) with lower cytotoxicity. The structure-activity relationships (SARs) of these caudatin analogs were also discussed.
DOI: 10.2174/1573406410666140902111326
PubMed: 25181984
Affiliations:
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Le document en format XML
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<term>Antiviral Agents (pharmacology)</term>
<term>Cell Survival (drug effects)</term>
<term>DNA Replication (drug effects)</term>
<term>DNA, Viral (biosynthesis)</term>
<term>Drug Design</term>
<term>Glycosides (chemical synthesis)</term>
<term>Glycosides (chemistry)</term>
<term>Glycosides (pharmacology)</term>
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<term>Hepatitis B virus (genetics)</term>
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<term>Steroids (chemistry)</term>
<term>Steroids (pharmacology)</term>
<term>Structure-Activity Relationship</term>
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<term>Virus de l'hépatite B (croissance et développement)</term>
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<front><div type="abstract" xml:lang="en">Thirty-nine caudatin analogs were designed and synthesized. Their anti-hepatitis B virus (HBV) activities were evaluated in vitro. Among them, twenty-three compounds showed much better anti-HBV activity than caudatin, and eleven compounds significantly inhibited the HBV DNA replication with IC50 values < 10 μM. Interestingly, three compounds (22, 28, 29) exhibited excellent activity against the secretion of HBsAg (IC50 = 63.02 μM, 52.81 μM, 56.08 μM), HBeAg (IC50 = 204.80 μM, 173.51 μM, 70.39 μM), along with HBV DNA replication (IC50 = 24.55 μM, 5.69 μM, 8.23 μM) with lower cytotoxicity. The structure-activity relationships (SARs) of these caudatin analogs were also discussed. </div>
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<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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<name sortKey="Wang, Li Jun" sort="Wang, Li Jun" uniqKey="Wang L" first="Li-Jun" last="Wang">Li-Jun Wang</name>
<name sortKey="Zhang, Xue Mei" sort="Zhang, Xue Mei" uniqKey="Zhang X" first="Xue-Mei" last="Zhang">Xue-Mei Zhang</name>
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