Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.
Identifieur interne : 002037 ( Main/Exploration ); précédent : 002036; suivant : 002038Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.
Auteurs : Rui-Hua Guo [République populaire de Chine] ; Quan Zhang ; Yun-Bao Ma ; Jie Luo ; Chang-An Geng ; Li-Jun Wang ; Xue-Mei Zhang ; Jun Zhou ; Zhi-Yong Jiang ; Ji-Jun ChenSource :
- European journal of medicinal chemistry [ 1768-3254 ] ; 2011.
Descripteurs français
- KwdFr :
- ADN viral (biosynthèse), 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, Quinolinone (), Quinolinone (pharmacologie), Quinolinone (synthèse chimique), Relation structure-activité, Réplication de l'ADN (), Virus de l'hépatite B (), Virus de l'hépatite B (génétique), Virus de l'hépatite B (métabolisme), Éléments activateurs (génétique) (génétique).
- MESH :
- biosynthèse : ADN viral.
- génétique : Virus de l'hépatite B, Éléments activateurs (génétique).
- 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, Quinolinone.
- synthèse chimique : Antiviraux, Quinolinone.
- Antiviraux, Cellules HepG2, Humains, Quinolinone, Relation structure-activité, Réplication de l'ADN, Virus de l'hépatite B.
English descriptors
- KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), DNA Replication (drug effects), DNA, Viral (biosynthesis), Enhancer Elements, Genetic (genetics), Hep G2 Cells, Hepatitis B Surface Antigens (metabolism), Hepatitis B e Antigens (metabolism), Hepatitis B virus (drug effects), Hepatitis B virus (genetics), Hepatitis B virus (metabolism), Humans, Quinolones (chemical synthesis), Quinolones (chemistry), Quinolones (pharmacology), Structure-Activity Relationship.
- MESH :
- chemical , biosynthesis : DNA, Viral.
- chemical , chemical synthesis : Antiviral Agents, Quinolones.
- chemical , chemistry : Antiviral Agents, Quinolones.
- chemical , metabolism : Hepatitis B Surface Antigens, Hepatitis B e Antigens.
- chemical , pharmacology : Antiviral Agents, Quinolones.
- drug effects : DNA Replication, Hepatitis B virus.
- genetics : Enhancer Elements, Genetic, Hepatitis B virus.
- metabolism : Hepatitis B virus.
- Hep G2 Cells, Humans, Structure-Activity Relationship.
Abstract
A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC(50) = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC(50) = 0.026 mM, SI > 51) and the replication of HBV DNA (IC(50) = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).
DOI: 10.1016/j.ejmech.2010.11.019
PubMed: 21145140
Affiliations:
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structure-activité</term><term>Réplication de l'ADN</term><term>Virus de l'hépatite B</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC(50) = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC(50) = 0.026 mM, SI > 51) and the replication of HBV DNA (IC(50) = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).</div></front></TEI><affiliations><list><country><li>République populaire de Chine</li></country></list><tree><noCountry><name sortKey="Chen, Ji Jun" sort="Chen, Ji Jun" uniqKey="Chen J" first="Ji-Jun" last="Chen">Ji-Jun Chen</name><name sortKey="Geng, Chang An" sort="Geng, Chang An" uniqKey="Geng C" first="Chang-An" last="Geng">Chang-An Geng</name><name sortKey="Jiang, Zhi Yong" sort="Jiang, Zhi Yong" uniqKey="Jiang Z" first="Zhi-Yong" last="Jiang">Zhi-Yong Jiang</name><name sortKey="Luo, Jie" sort="Luo, Jie" uniqKey="Luo J" first="Jie" last="Luo">Jie Luo</name><name sortKey="Ma, Yun Bao" sort="Ma, Yun Bao" uniqKey="Ma Y" first="Yun-Bao" last="Ma">Yun-Bao Ma</name><name sortKey="Wang, Li Jun" sort="Wang, Li Jun" uniqKey="Wang L" first="Li-Jun" last="Wang">Li-Jun Wang</name><name sortKey="Zhang, Quan" sort="Zhang, Quan" uniqKey="Zhang Q" first="Quan" last="Zhang">Quan Zhang</name><name sortKey="Zhang, Xue Mei" sort="Zhang, Xue Mei" uniqKey="Zhang X" first="Xue-Mei" last="Zhang">Xue-Mei Zhang</name><name sortKey="Zhou, Jun" sort="Zhou, Jun" uniqKey="Zhou J" first="Jun" last="Zhou">Jun Zhou</name></noCountry><country name="République populaire de Chine"><noRegion><name sortKey="Guo, Rui Hua" sort="Guo, Rui Hua" uniqKey="Guo R" first="Rui-Hua" last="Guo">Rui-Hua Guo</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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