SrasV1, Main, Exploration, bibRecord, 001F59

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

Identifieur interne : 001F59 ( Main/Exploration ); précédent : 001F58; suivant : 001F60

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 [République populaire de Chine] ; Yun-Bao Ma [République populaire de Chine] ; Xiao-Yan Huang [République populaire de Chine] ; JIE LUO [République populaire de Chine] ; HAO CHEN [République populaire de Chine] ; Rui-Hua Guo [République populaire de Chine] ; Xue-Mei Zhang [République populaire de Chine] ; Ji-Jun Chen [République populaire de Chine]

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.

Affiliations:

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

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Le document en format XML

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<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>
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<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>
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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>
</front>
</TEI>
<affiliations><list><country><li>République populaire de Chine</li>
</country>
<settlement><li>Pékin</li>
</settlement>
</list>
<tree><country name="République populaire de Chine"><noRegion><name sortKey="Wang, Li Jun" sort="Wang, Li Jun" uniqKey="Wang L" first="Li-Jun" last="Wang">Li-Jun Wang</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="Geng, Chang An" sort="Geng, Chang An" uniqKey="Geng C" first="Chang-An" last="Geng">Chang-An Geng</name>
<name sortKey="Guo, Rui Hua" sort="Guo, Rui Hua" uniqKey="Guo R" first="Rui-Hua" last="Guo">Rui-Hua Guo</name>
<name sortKey="Guo, Rui Hua" sort="Guo, Rui Hua" uniqKey="Guo R" first="Rui-Hua" last="Guo">Rui-Hua Guo</name>
<name sortKey="Hao Chen" sort="Hao Chen" uniqKey="Hao Chen" last="Hao Chen">HAO CHEN</name>
<name sortKey="Hao Chen" sort="Hao Chen" uniqKey="Hao Chen" last="Hao Chen">HAO 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="Jie Luo" sort="Jie Luo" uniqKey="Jie Luo" last="Jie 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, Xue Mei" sort="Zhang, Xue Mei" uniqKey="Zhang X" first="Xue-Mei" last="Zhang">Xue-Mei Zhang</name>
</country>
</tree>
</affiliations>
</record>

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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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