SrasV1, Main, Exploration, bibRecord, 001557

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

Identifieur interne : 001557 ( Main/Exploration ); précédent : 001556; suivant : 001558

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

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

Source :

Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2014.

RBID : pubmed:24731274

Descripteurs français

KwdFr :
- ADN viral (biosynthèse), ADN viral (génétique), Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Diterpènes (), Diterpènes (pharmacologie), Diterpènes (synthèse chimique), Produits biologiques, Relation structure-activité, Réplication de l'ADN (), Réplication virale (), Virus de l'hépatite B (), Virus de l'hépatite B (génétique), Virus de l'hépatite B (physiologie).
MESH :
- biosynthèse : ADN viral.
- génétique : ADN viral, Virus de l'hépatite B.
- pharmacologie : Antiviraux, Diterpènes.
- physiologie : Virus de l'hépatite B.
- synthèse chimique : Antiviraux, Diterpènes.
- Antiviraux, Diterpènes, Produits biologiques, Relation structure-activité, Réplication de l'ADN, Réplication virale, Virus de l'hépatite B.

English descriptors

KwdEn :
- Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Biological Products, DNA Replication (drug effects), DNA, Viral (biosynthesis), DNA, Viral (genetics), Diterpenes (chemical synthesis), Diterpenes (chemistry), Diterpenes (pharmacology), Hepatitis B virus (drug effects), Hepatitis B virus (genetics), Hepatitis B virus (physiology), Structure-Activity Relationship, Virus Replication (drug effects).
MESH :
- chemical , biosynthesis : DNA, Viral.
- chemical , chemical synthesis : Antiviral Agents, Diterpenes.
- chemical , chemistry : Antiviral Agents, Diterpenes.
- chemical , genetics : DNA, Viral.
- chemical , pharmacology : Antiviral Agents, Diterpenes.
- chemical : Biological Products.
- drug effects : DNA Replication, Hepatitis B virus, Virus Replication.
- genetics : Hepatitis B virus.
- physiology : Hepatitis B virus.
- Structure-Activity Relationship.

Abstract

Dehydroandrographolide and andrographolide, two natural diterpenoids isolated from Andrographis paniculata possessed activity against HBV DNA replication with IC50 values of 22.58 and 54.07μM and low SI values of 8.7 and 3.7 in our random assay. Consequently, 48 derivatives of dehydroandrographolide and andrographolide were synthesized and evaluated for their anti-HBV properties to yield a series of active derivatives with lower cytotoxicity, including 14 derivatives against HBsAg secretion, 19 derivatives against HBeAg secretion and 38 derivatives against HBV DNA replication. Interestingly, compound 4e could inhibit not only HBsAg and HBeAg secretions but also HBV DNA replication with SI values of 20.3, 125.0 and 104.9. Furthermore, the most active compound 2c with SI value higher than 165.1 inhibiting HBV DNA replication was revealed with the optimal logP value of 1.78 and logD values. Structure-activity relationships (SARs) of the derivatives were disclosed for guiding the future research toward the discovery of new anti-HBV drugs.

DOI: 10.1016/j.bmcl.2014.03.060
PubMed: 24731274

Affiliations:

Le document en format XML

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<front><div type="abstract" xml:lang="en">Dehydroandrographolide and andrographolide, two natural diterpenoids isolated from Andrographis paniculata possessed activity against HBV DNA replication with IC50 values of 22.58 and 54.07μM and low SI values of 8.7 and 3.7 in our random assay. Consequently, 48 derivatives of dehydroandrographolide and andrographolide were synthesized and evaluated for their anti-HBV properties to yield a series of active derivatives with lower cytotoxicity, including 14 derivatives against HBsAg secretion, 19 derivatives against HBeAg secretion and 38 derivatives against HBV DNA replication. Interestingly, compound 4e could inhibit not only HBsAg and HBeAg secretions but also HBV DNA replication with SI values of 20.3, 125.0 and 104.9. Furthermore, the most active compound 2c with SI value higher than 165.1 inhibiting HBV DNA replication was revealed with the optimal logP value of 1.78 and logD values. Structure-activity relationships (SARs) of the derivatives were disclosed for guiding the future research toward the discovery of new anti-HBV drugs. </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>
<name sortKey="Liang, Wen Juan" sort="Liang, Wen Juan" uniqKey="Liang W" first="Wen-Juan" last="Liang">Wen-Juan Liang</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>
<name sortKey="Zhao, Yong" sort="Zhao, Yong" uniqKey="Zhao Y" first="Yong" last="Zhao">Yong Zhao</name>
</country>
</tree>
</affiliations>
</record>

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{{Explor lien
   |wiki=    Sante
   |area=    SrasV1
   |flux=    Main
   |étape=   Exploration
   |type=    RBID
   |clé=     pubmed:24731274
   |texte=   Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents.
}}

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

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

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