SrasV1, Main, Exploration, bibRecord, 002F39

Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors

Identifieur interne : 002F39 ( Main/Exploration ); précédent : 002F38; suivant : 002F40

Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors

Auteurs : Iou-Jiun Kang [Taïwan] ; Li-Wen Wang [Taïwan] ; Sheng-Ju Hsu [Taïwan] ; Chung-Chi Lee [Taïwan] ; Yen-Chun Lee [Taïwan] ; Yen-Shian Wu [Taïwan] ; Andrew Yueh [Taïwan] ; Jing-Chyi Wang [Taïwan] ; Tsu-An Hsu [Taïwan] ; Yu-Sheng Chao [Taïwan] ; Jyh-Haur Chern [Taïwan]

Source :

Bioorganic & medicinal chemistry letters : (Print) [ 0960-894X ] ; 2009.

RBID : Pascal:10-0093032

Descripteurs français

Pascal (Inist)
- Synthèse chimique, Thiourées, Antiviral, Virus hépatite C, Relation structure activité, Dérivé du benzène, Ether, Longueur chaîne, Dérivé du carbazole, Hétérocycle azote, Composé tricyclique, Composé aromatique, Composé aliphatique, In vitro.

English descriptors

KwdEn :
- Aliphatic compound, Antiviral, Aromatic compound, Benzene derivatives, Carbazole derivatives, Chain length, Chemical synthesis, Ether, Hepatitis C virus, In vitro, Nitrogen heterocycle, Structure activity relation, Thioureas, Tricyclic compound.

Abstract

A novel class of arylthiourea HCV inhibitors bearing various functionalities, such as cyclic urea, cyclic thiourea, urea, and thiourea, on the alkyl linker were designed and synthesized. Herein we report the synthesis and structure-activity relationships (SARs) of this novel class of arylthiourea derivatives that showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon assay. Among compounds tested, the new carbazole derivative 64, which has an eight-carbon linkage between the phenyl and carbazole rings and a tolyl group at the N-9 position of carbazole, was found to possess strong anti-HCV activity (EC₅₀=0.031 μM), lower cytotoxicity (CC₅₀ >50 μM), and higher selectivity index (SI >1612) compared to its derivatives.

Affiliations:

Taïwan

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

to stream PascalFrancis, to step Corpus: 000172
to stream PascalFrancis, to step Curation: 000816
to stream PascalFrancis, to step Checkpoint: 000221
to stream Main, to step Merge: 002F98
to stream Main, to step Curation: 002F39

Le document en format XML

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<author><name sortKey="Chern, Jyh Haur" sort="Chern, Jyh Haur" uniqKey="Chern J" first="Jyh-Haur" last="Chern">Jyh-Haur Chern</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road</s1>
<s2>Zhunan Town, Miaoli County 350</s2>
<s3>TWN</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>
<sZ>10 aut.</sZ>
<sZ>11 aut.</sZ>
</inist:fA14>
<country>Taïwan</country>
<wicri:noRegion>Zhunan Town, Miaoli County 350</wicri:noRegion>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">Bioorganic & medicinal chemistry letters : (Print)</title>
<title level="j" type="abbreviated">Bioorg. med. chem. lett. : (Print)</title>
<idno type="ISSN">0960-894X</idno>
<imprint><date when="2009">2009</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><title level="j" type="main">Bioorganic & medicinal chemistry letters : (Print)</title>
<title level="j" type="abbreviated">Bioorg. med. chem. lett. : (Print)</title>
<idno type="ISSN">0960-894X</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Aliphatic compound</term>
<term>Antiviral</term>
<term>Aromatic compound</term>
<term>Benzene derivatives</term>
<term>Carbazole derivatives</term>
<term>Chain length</term>
<term>Chemical synthesis</term>
<term>Ether</term>
<term>Hepatitis C virus</term>
<term>In vitro</term>
<term>Nitrogen heterocycle</term>
<term>Structure activity relation</term>
<term>Thioureas</term>
<term>Tricyclic compound</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Synthèse chimique</term>
<term>Thiourées</term>
<term>Antiviral</term>
<term>Virus hépatite C</term>
<term>Relation structure activité</term>
<term>Dérivé du benzène</term>
<term>Ether</term>
<term>Longueur chaîne</term>
<term>Dérivé du carbazole</term>
<term>Hétérocycle azote</term>
<term>Composé tricyclique</term>
<term>Composé aromatique</term>
<term>Composé aliphatique</term>
<term>In vitro</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">A novel class of arylthiourea HCV inhibitors bearing various functionalities, such as cyclic urea, cyclic thiourea, urea, and thiourea, on the alkyl linker were designed and synthesized. Herein we report the synthesis and structure-activity relationships (SARs) of this novel class of arylthiourea derivatives that showed potent inhibitory activities against HCV in the cell-based subgenomic HCV replicon assay. Among compounds tested, the new carbazole derivative 64, which has an eight-carbon linkage between the phenyl and carbazole rings and a tolyl group at the N-9 position of carbazole, was found to possess strong anti-HCV activity (EC<sub>50</sub>
=0.031 μM), lower cytotoxicity (CC<sub>50</sub>
 >50 μM), and higher selectivity index (SI >1612) compared to its derivatives.</div>
</front>
</TEI>
<affiliations><list><country><li>Taïwan</li>
</country>
</list>
<tree><country name="Taïwan"><noRegion><name sortKey="Kang, Iou Jiun" sort="Kang, Iou Jiun" uniqKey="Kang I" first="Iou-Jiun" last="Kang">Iou-Jiun Kang</name>
</noRegion>
<name sortKey="Chao, Yu Sheng" sort="Chao, Yu Sheng" uniqKey="Chao Y" first="Yu-Sheng" last="Chao">Yu-Sheng Chao</name>
<name sortKey="Chern, Jyh Haur" sort="Chern, Jyh Haur" uniqKey="Chern J" first="Jyh-Haur" last="Chern">Jyh-Haur Chern</name>
<name sortKey="Hsu, Sheng Ju" sort="Hsu, Sheng Ju" uniqKey="Hsu S" first="Sheng-Ju" last="Hsu">Sheng-Ju Hsu</name>
<name sortKey="Hsu, Tsu An" sort="Hsu, Tsu An" uniqKey="Hsu T" first="Tsu-An" last="Hsu">Tsu-An Hsu</name>
<name sortKey="Lee, Chung Chi" sort="Lee, Chung Chi" uniqKey="Lee C" first="Chung-Chi" last="Lee">Chung-Chi Lee</name>
<name sortKey="Lee, Yen Chun" sort="Lee, Yen Chun" uniqKey="Lee Y" first="Yen-Chun" last="Lee">Yen-Chun Lee</name>
<name sortKey="Wang, Jing Chyi" sort="Wang, Jing Chyi" uniqKey="Wang J" first="Jing-Chyi" last="Wang">Jing-Chyi Wang</name>
<name sortKey="Wang, Li Wen" sort="Wang, Li Wen" uniqKey="Wang L" first="Li-Wen" last="Wang">Li-Wen Wang</name>
<name sortKey="Wu, Yen Shian" sort="Wu, Yen Shian" uniqKey="Wu Y" first="Yen-Shian" last="Wu">Yen-Shian Wu</name>
<name sortKey="Yueh, Andrew" sort="Yueh, Andrew" uniqKey="Yueh A" first="Andrew" last="Yueh">Andrew Yueh</name>
</country>
</tree>
</affiliations>
</record>

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Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors

Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors

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