SrasV1, PascalFrancis, Corpus, bibRecord, 000051

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

Identifieur interne : 000051 ( PascalFrancis/Corpus ); précédent : 000050; suivant : 000052

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

Auteurs : Li-Jun Wang ; 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 [ 0968-0896 ] ; 2012.

RBID : Pascal:12-0356332

Descripteurs français

Pascal (Inist)
- Synthèse chimique, Relation structure activité, Activité biologique, Antiviral, Virus hépatite B, Dérivé du prégnane, Stéroïde, Caudatine dérivé.

English descriptors

KwdEn :
- Antiviral, Biological activity, Chemical synthesis, Hepatitis B virus, Pregnane derivatives, Steroid, Structure activity relation.

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 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC₅₀ 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 (IC₅₀ = 18.68 μM, 21.71 μM), HBeAg (IC₅₀ = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC₅₀ = 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.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

A01	`01`	`1`		`@0 0968-0896`
A03		`1`		`@0 Bioorg. med. chem.`
A05				`@2 20`
A06				`@2 9`
A08	`01`	`1`	`ENG`	`@1 Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents`
A11	`01`	`1`		`@1 WANG (Li-Jun)`
A11	`02`	`1`		`@1 GENG (Chang-An)`
A11	`03`	`1`		`@1 MA (Yun-Bao)`
A11	`04`	`1`		`@1 HUANG (Xiao-Yan)`
A11	`05`	`1`		`@1 JIE LUO`
A11	`06`	`1`		`@1 HAO CHEN`
A11	`07`	`1`		`@1 GUO (Rui-Hua)`
A11	`08`	`1`		`@1 ZHANG (Xue-Mei)`
A11	`09`	`1`		`@1 CHEN (Ji-Jun)`
A14	`01`			`@1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences @2 Kunming 650201 @3 CHN @Z 1 aut. @Z 2 aut. @Z 3 aut. @Z 4 aut. @Z 5 aut. @Z 6 aut. @Z 7 aut. @Z 8 aut. @Z 9 aut.`
A14	`02`			`@1 Graduate University of the Chinese Academy of Sciences @2 Beijing 100049 @3 CHN @Z 1 aut. @Z 6 aut. @Z 7 aut.`
A20				`@1 2877-2888`
A21				`@1 2012`
A23	`01`			`@0 ENG`
A43	`01`			`@1 INIST @2 26564 @5 354000509867520130`
A44				`@0 0000 @1 © 2012 INIST-CNRS. All rights reserved.`
A47	`01`	`1`		`@0 12-0356332`
A60				`@1 P`
A61				`@0 A`
A64	`01`	`1`		`@0 Bioorganic & medicinal chemistry`
A66	`01`			`@0 NLD`
A99				`@0 1/4 p. ref. et notes`
C01	`01`		`ENG`	@0 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 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC₅₀ 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 (IC₅₀ = 18.68 μM, 21.71 μM), HBeAg (IC₅₀ = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC₅₀ = 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.
C02	`01`	`X`		`@0 002B02S05`
C03	`01`	`X`	`FRE`	`@0 Synthèse chimique @5 01`
C03	`01`	`X`	`ENG`	`@0 Chemical synthesis @5 01`
C03	`01`	`X`	`SPA`	`@0 Síntesis química @5 01`
C03	`02`	`X`	`FRE`	`@0 Relation structure activité @5 02`
C03	`02`	`X`	`ENG`	`@0 Structure activity relation @5 02`
C03	`02`	`X`	`SPA`	`@0 Relación estructura actividad @5 02`
C03	`03`	`X`	`FRE`	`@0 Activité biologique @5 03`
C03	`03`	`X`	`ENG`	`@0 Biological activity @5 03`
C03	`03`	`X`	`SPA`	`@0 Actividad biológica @5 03`
C03	`04`	`X`	`FRE`	`@0 Antiviral @5 04`
C03	`04`	`X`	`ENG`	`@0 Antiviral @5 04`
C03	`04`	`X`	`SPA`	`@0 Antiviral @5 04`
C03	`05`	`X`	`FRE`	`@0 Virus hépatite B @2 NW @5 05`
C03	`05`	`X`	`ENG`	`@0 Hepatitis B virus @2 NW @5 05`
C03	`05`	`X`	`SPA`	`@0 Hepatitis B virus @2 NW @5 05`
C03	`06`	`X`	`FRE`	`@0 Dérivé du prégnane @2 FR @5 23`
C03	`06`	`X`	`ENG`	`@0 Pregnane derivatives @2 FR @5 23`
C03	`07`	`X`	`FRE`	`@0 Stéroïde @5 24`
C03	`07`	`X`	`ENG`	`@0 Steroid @5 24`
C03	`07`	`X`	`SPA`	`@0 Esteroide @5 24`
C03	`08`	`X`	`FRE`	`@0 Caudatine dérivé @4 INC @5 86`
C07	`01`	`X`	`FRE`	`@0 Orthohepadnavirus @2 NW`
C07	`01`	`X`	`ENG`	`@0 Orthohepadnavirus @2 NW`
C07	`01`	`X`	`SPA`	`@0 Orthohepadnavirus @2 NW`
C07	`02`	`X`	`FRE`	`@0 Hepadnaviridae @2 NW`
C07	`02`	`X`	`ENG`	`@0 Hepadnaviridae @2 NW`
C07	`02`	`X`	`SPA`	`@0 Hepadnaviridae @2 NW`
C07	`03`	`X`	`FRE`	`@0 Virus @2 NW`
C07	`03`	`X`	`ENG`	`@0 Virus @2 NW`
C07	`03`	`X`	`SPA`	`@0 Virus @2 NW`
N21				`@1 275`
N44	`01`			`@1 OTO`
N82				`@1 OTO`

Format Inist (serveur)

NO :	PASCAL 12-0356332 INIST
ET :	Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents
AU :	WANG (Li-Jun); GENG (Chang-An); MA (Yun-Bao); HUANG (Xiao-Yan); JIE LUO; HAO CHEN; GUO (Rui-Hua); ZHANG (Xue-Mei); CHEN (Ji-Jun)
AF :	State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences/Kunming 650201/Chine (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut., 9 aut.); Graduate University of the Chinese Academy of Sciences/Beijing 100049/Chine (1 aut., 6 aut., 7 aut.)
DT :	Publication en série; Niveau analytique
SO :	Bioorganic & medicinal chemistry; ISSN 0968-0896; Pays-Bas; Da. 2012; Vol. 20; No. 9; Pp. 2877-2888
LA :	Anglais
EA :	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 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC₅₀ 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 (IC₅₀ = 18.68 μM, 21.71 μM), HBeAg (IC₅₀ = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC₅₀ = 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.
CC :	002B02S05
FD :	Synthèse chimique; Relation structure activité; Activité biologique; Antiviral; Virus hépatite B; Dérivé du prégnane; Stéroïde; Caudatine dérivé
FG :	Orthohepadnavirus; Hepadnaviridae; Virus
ED :	Chemical synthesis; Structure activity relation; Biological activity; Antiviral; Hepatitis B virus; Pregnane derivatives; Steroid
EG :	Orthohepadnavirus; Hepadnaviridae; Virus
SD :	Síntesis química; Relación estructura actividad; Actividad biológica; Antiviral; Hepatitis B virus; Esteroide
LO :	INIST-26564.354000509867520130
ID :	12-0356332

Links to Exploration step

Pascal:12-0356332

Le document en format XML

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<author><name sortKey="Zhang, Xue Mei" sort="Zhang, Xue Mei" uniqKey="Zhang X" first="Xue-Mei" last="Zhang">Xue-Mei Zhang</name>
<affiliation><inist:fA14 i1="01"><s1>State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences</s1>
<s2>Kunming 650201</s2>
<s3>CHN</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>8 aut.</sZ>
<sZ>9 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Chen, Ji Jun" sort="Chen, Ji Jun" uniqKey="Chen J" first="Ji-Jun" last="Chen">Ji-Jun Chen</name>
<affiliation><inist:fA14 i1="01"><s1>State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences</s1>
<s2>Kunming 650201</s2>
<s3>CHN</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>8 aut.</sZ>
<sZ>9 aut.</sZ>
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<series><title level="j" type="main">Bioorganic & medicinal chemistry</title>
<title level="j" type="abbreviated">Bioorg. med. chem.</title>
<idno type="ISSN">0968-0896</idno>
<imprint><date when="2012">2012</date>
</imprint>
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<seriesStmt><title level="j" type="main">Bioorganic & medicinal chemistry</title>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral</term>
<term>Biological activity</term>
<term>Chemical synthesis</term>
<term>Hepatitis B virus</term>
<term>Pregnane derivatives</term>
<term>Steroid</term>
<term>Structure activity relation</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Synthèse chimique</term>
<term>Relation structure activité</term>
<term>Activité biologique</term>
<term>Antiviral</term>
<term>Virus hépatite B</term>
<term>Dérivé du prégnane</term>
<term>Stéroïde</term>
<term>Caudatine dérivé</term>
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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 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC<sub>50</sub>
 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<sub>50</sub>
 = 18.68 μM, 21.71 μM), HBeAg (IC<sub>50</sub>
 = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC<sub>50</sub>
 = 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>
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<sZ>6 aut.</sZ>
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<fA14 i1="02"><s1>Graduate University of the Chinese Academy of Sciences</s1>
<s2>Beijing 100049</s2>
<s3>CHN</s3>
<sZ>1 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>7 aut.</sZ>
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 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<sub>50</sub>
 = 18.68 μM, 21.71 μM), HBeAg (IC<sub>50</sub>
 = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC<sub>50</sub>
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<server><NO>PASCAL 12-0356332 INIST</NO>
<ET>Synthesis, structure-activity relationships and biological evaluation of caudatin derivatives as novel anti-hepatitis B virus agents</ET>
<AU>WANG (Li-Jun); GENG (Chang-An); MA (Yun-Bao); HUANG (Xiao-Yan); JIE LUO; HAO CHEN; GUO (Rui-Hua); ZHANG (Xue-Mei); CHEN (Ji-Jun)</AU>
<AF>State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences/Kunming 650201/Chine (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut., 9 aut.); Graduate University of the Chinese Academy of Sciences/Beijing 100049/Chine (1 aut., 6 aut., 7 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>Bioorganic & medicinal chemistry; ISSN 0968-0896; Pays-Bas; Da. 2012; Vol. 20; No. 9; Pp. 2877-2888</SO>
<LA>Anglais</LA>
<EA>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 3-0-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e-2h, 21, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC<sub>50</sub>
 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<sub>50</sub>
 = 18.68 μM, 21.71 μM), HBeAg (IC<sub>50</sub>
 = 13.16 μM, 33.73 μM), but also HBV DNA replication (IC<sub>50</sub>
 = 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.</EA>
<CC>002B02S05</CC>
<FD>Synthèse chimique; Relation structure activité; Activité biologique; Antiviral; Virus hépatite B; Dérivé du prégnane; Stéroïde; Caudatine dérivé</FD>
<FG>Orthohepadnavirus; Hepadnaviridae; Virus</FG>
<ED>Chemical synthesis; Structure activity relation; Biological activity; Antiviral; Hepatitis B virus; Pregnane derivatives; Steroid</ED>
<EG>Orthohepadnavirus; Hepadnaviridae; Virus</EG>
<SD>Síntesis química; Relación estructura actividad; Actividad biológica; Antiviral; Hepatitis B virus; Esteroide</SD>
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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

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