SrasV1, Main, Exploration, bibRecord, 001C45

Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents.

Identifieur interne : 001C45 ( Main/Exploration ); précédent : 001C44; suivant : 001C46

Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents.

Auteurs : Li-Jun Wang [République populaire de Chine] ; Chang-An Geng ; Yun-Bao Ma ; Xiao-Yan Huang ; Jie Luo ; Hao Chen ; Rui-Hua Guo ; Xue-Mei Zhang ; Ji-Jun Chen

Source :

Bioorganic & medicinal chemistry [ 1464-3391 ] ; 2012.

RBID : pubmed:22472044

Descripteurs français

KwdFr :
- Antigènes de surface du virus de l'hépatite B (métabolisme), Antigènes e du virus de l'hépatite virale B (métabolisme), Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Cellules HepG2, Humains, Hétérosides (), Hétérosides (pharmacologie), Hétérosides (synthèse chimique), Relation structure-activité, Réplication de l'ADN (), Stéroïdes (), Stéroïdes (pharmacologie), Stéroïdes (synthèse chimique), Virus de l'hépatite B (), Virus de l'hépatite B (métabolisme).
MESH :
- métabolisme : Antigènes de surface du virus de l'hépatite B, Antigènes e du virus de l'hépatite virale B, Virus de l'hépatite B.
- pharmacologie : Antiviraux, Hétérosides, Stéroïdes.
- synthèse chimique : Antiviraux, Hétérosides, Stéroïdes.
- Antiviraux, Cellules HepG2, Humains, Hétérosides, Relation structure-activité, Réplication de l'ADN, Stéroïdes, Virus de l'hépatite B.

English descriptors

KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), DNA Replication (drug effects), Glycosides (chemical synthesis), Glycosides (chemistry), Glycosides (pharmacology), Hep G2 Cells, Hepatitis B Surface Antigens (metabolism), Hepatitis B e Antigens (metabolism), Hepatitis B virus (drug effects), Hepatitis B virus (metabolism), Humans, Steroids (chemical synthesis), Steroids (chemistry), Steroids (pharmacology), Structure-Activity Relationship.
MESH :
- chemical , chemical synthesis : Antiviral Agents, Glycosides, Steroids.
- chemical , chemistry : Antiviral Agents, Glycosides, Steroids.
- chemical , metabolism : Hepatitis B Surface Antigens, Hepatitis B e Antigens.
- chemical , pharmacology : Antiviral Agents, Glycosides, Steroids.
- drug effects : DNA Replication, Hepatitis B virus.
- metabolism : Hepatitis B virus.
- Hep G2 Cells, Humans, Structure-Activity Relationship.

Abstract

A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC(50) values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC(50)=18.68 μM, 21.71 μM), HBeAg (IC(50)=13.16 μM, 33.73 μM), but also HBV DNA replication (IC(50)=7.48 μM, 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.

DOI: 10.1016/j.bmc.2012.03.023
PubMed: 22472044

Affiliations:

République populaire de Chine

Le document en format XML

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<front><div type="abstract" xml:lang="en">A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC(50) values in the range of 2.82-7.48 μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC(50)=18.68 μM, 21.71 μM), HBeAg (IC(50)=13.16 μM, 33.73 μM), but also HBV DNA replication (IC(50)=7.48 μM, 3.63 μM). The structure-activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents.</div>
</front>
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Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents.

Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

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