Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors
Identifieur interne : 004D51 ( Main/Exploration ); précédent : 004D50; suivant : 004D52Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors
Auteurs : Li-Rung Chen [Taïwan] ; Yu-Chin Wang [Taïwan] ; YI WEN LIN [Taïwan] ; Shan-Yen Chou [Taïwan] ; Shyh-Fong Chen [Taïwan] ; LEE TAI LIU [Taïwan] ; Ying-Ta Wu [Taïwan] ; Chih-Jung Kuo [Taïwan] ; Tom Shieh-Shung Chen [Taïwan] ; Shin-Hun Juang [Taïwan]Source :
- Bioorganic & medicinal chemistry letters : (Print) [ 0960-894X ] ; 2005.
Descripteurs français
- KwdFr :
- Activation enzymatique, Chymotrypsine (pharmacologie), Cysteine endopeptidases, Endopeptidases, Humains, Inhibiteurs de protéases (), Inhibiteurs de protéases (pharmacologie), Inhibiteurs de protéases (synthèse chimique), Isatine (analogues et dérivés), Isatine (pharmacologie), Isatine (synthèse chimique), Papaïne (pharmacologie), Protéines virales (antagonistes et inhibiteurs), Relation structure-activité, Simulation numérique, Sites de fixation, Spécificité du substrat, Structure moléculaire, Transfert d'énergie par résonance de fluorescence, Trypsine (pharmacologie), Virus du SRAS (enzymologie).
- MESH :
- analogues et dérivés : Isatine.
- antagonistes et inhibiteurs : Protéines virales.
- enzymologie : Virus du SRAS.
- pharmacologie : Chymotrypsine, Inhibiteurs de protéases, Isatine, Papaïne, Trypsine.
- synthèse chimique : Inhibiteurs de protéases, Isatine.
- Pascal (Inist)
- Activation enzymatique, Cysteine endopeptidases, Endopeptidases, Humains, Inhibiteurs de protéases, Relation structure-activité, Simulation numérique, Sites de fixation, Spécificité du substrat, Structure moléculaire, Synthèse chimique, Isatine, Transfert d'énergie par résonance de fluorescence, Virus syndrome respiratoire aigu sévère, Inhibiteur protease, Activité biologique, In vitro, Sélectivité, Peptidases, Antiviral, Modèle moléculaire, Complexe enzyme inhibiteur, Indole dérivé, Inhibiteur enzyme, Modélisation, Indole-2,3-dione(1-[benzo[b]thién-2-ylméthyl]-5-iodo), Benzo[b]thiophène dérivé, benzothiophene.
English descriptors
- KwdEn :
- Antiviral, Binding Sites, Biological activity, Chemical synthesis, Chymotrypsin (pharmacology), Computer Simulation, Cysteine Endopeptidases, Endopeptidases, Enzyme Activation, Enzyme inhibitor, Fluorescence Resonance Energy Transfer, Humans, In vitro, Indole derivatives, Inhibitor enzyme complex, Isatin (analogs & derivatives), Isatin (chemical synthesis), Isatin (pharmacology), Modeling, Molecular Structure, Molecular model, Papain (pharmacology), Peptidases, Protease Inhibitors (chemical synthesis), Protease Inhibitors (chemistry), Protease Inhibitors (pharmacology), Protease inhibitor, SARS Virus (enzymology), Selectivity, Severe acute respiratory syndrome virus, Structure-Activity Relationship, Substrate Specificity, Trypsin (pharmacology), Viral Proteins (antagonists & inhibitors).
- MESH :
- chemical , analogs & derivatives : Isatin.
- chemical , antagonists & inhibitors : Viral Proteins.
- chemical , chemical synthesis : Isatin, Protease Inhibitors.
- chemical , chemistry : Protease Inhibitors.
- chemical , pharmacology : Chymotrypsin, Isatin, Papain, Protease Inhibitors, Trypsin.
- enzymology : SARS Virus.
- Binding Sites, Computer Simulation, Cysteine Endopeptidases, Endopeptidases, Enzyme Activation, Fluorescence Resonance Energy Transfer, Humans, Molecular Structure, Structure-Activity Relationship, Substrate Specificity.
Abstract
N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.
Affiliations:
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inhibitors</title><author><name sortKey="Chen, Li Rung" sort="Chen, Li Rung" uniqKey="Chen L" first="Li-Rung" last="Chen">Li-Rung Chen</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Wang, Yu Chin" sort="Wang, Yu Chin" uniqKey="Wang Y" first="Yu-Chin" last="Wang">Yu-Chin Wang</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Yi Wen Lin" sort="Yi Wen Lin" uniqKey="Yi Wen Lin" last="Yi Wen Lin">YI WEN LIN</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Chou, Shan Yen" sort="Chou, Shan Yen" uniqKey="Chou S" first="Shan-Yen" last="Chou">Shan-Yen Chou</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Chen, Shyh Fong" sort="Chen, Shyh Fong" uniqKey="Chen S" first="Shyh-Fong" last="Chen">Shyh-Fong Chen</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Lee Tai Liu" sort="Lee Tai Liu" uniqKey="Lee Tai Liu" last="Lee Tai Liu">LEE TAI LIU</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Wu, Ying Ta" sort="Wu, Ying Ta" uniqKey="Wu Y" first="Ying-Ta" last="Wu">Ying-Ta Wu</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Institute of Biological Chemistry and the Genomic Research Center, Academia Sinica</s1><s2>Nang Gang 11529, Taipei</s2><s3>TWN</s3><sZ>7 aut.</sZ><sZ>8 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Nang Gang 11529, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Kuo, Chih Jung" sort="Kuo, Chih Jung" uniqKey="Kuo C" first="Chih-Jung" last="Kuo">Chih-Jung Kuo</name><affiliation wicri:level="1"><inist:fA14 i1="02"><s1>Institute of Biological Chemistry and the Genomic Research Center, Academia Sinica</s1><s2>Nang Gang 11529, Taipei</s2><s3>TWN</s3><sZ>7 aut.</sZ><sZ>8 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Nang Gang 11529, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Chen, Tom Shieh Shung" sort="Chen, Tom Shieh Shung" uniqKey="Chen T" first="Tom Shieh-Shung" last="Chen">Tom Shieh-Shung Chen</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</wicri:noRegion></affiliation></author><author><name sortKey="Juang, Shin Hun" sort="Juang, Shin Hun" uniqKey="Juang S" first="Shin-Hun" last="Juang">Shin-Hun Juang</name><affiliation wicri:level="1"><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1><s2>Xi Zhi 221, Taipei</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>9 aut.</sZ><sZ>10 aut.</sZ></inist:fA14><country>Taïwan</country><wicri:noRegion>Xi Zhi 221, Taipei</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="2005">2005</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>Antiviral</term><term>Binding Sites</term><term>Biological activity</term><term>Chemical synthesis</term><term>Chymotrypsin (pharmacology)</term><term>Computer Simulation</term><term>Cysteine Endopeptidases</term><term>Endopeptidases</term><term>Enzyme Activation</term><term>Enzyme inhibitor</term><term>Fluorescence Resonance Energy Transfer</term><term>Humans</term><term>In vitro</term><term>Indole derivatives</term><term>Inhibitor enzyme complex</term><term>Isatin (analogs & derivatives)</term><term>Isatin (chemical synthesis)</term><term>Isatin (pharmacology)</term><term>Modeling</term><term>Molecular Structure</term><term>Molecular model</term><term>Papain (pharmacology)</term><term>Peptidases</term><term>Protease Inhibitors (chemical synthesis)</term><term>Protease Inhibitors (chemistry)</term><term>Protease Inhibitors (pharmacology)</term><term>Protease inhibitor</term><term>SARS Virus (enzymology)</term><term>Selectivity</term><term>Severe acute respiratory syndrome virus</term><term>Structure-Activity Relationship</term><term>Substrate Specificity</term><term>Trypsin (pharmacology)</term><term>Viral Proteins (antagonists & inhibitors)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Activation enzymatique</term><term>Chymotrypsine (pharmacologie)</term><term>Cysteine endopeptidases</term><term>Endopeptidases</term><term>Humains</term><term>Inhibiteurs de protéases ()</term><term>Inhibiteurs de protéases (pharmacologie)</term><term>Inhibiteurs de protéases (synthèse chimique)</term><term>Isatine (analogues et dérivés)</term><term>Isatine (pharmacologie)</term><term>Isatine (synthèse chimique)</term><term>Papaïne (pharmacologie)</term><term>Protéines virales (antagonistes et inhibiteurs)</term><term>Relation structure-activité</term><term>Simulation numérique</term><term>Sites de fixation</term><term>Spécificité du substrat</term><term>Structure moléculaire</term><term>Transfert d'énergie par résonance de fluorescence</term><term>Trypsine (pharmacologie)</term><term>Virus du SRAS (enzymologie)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Isatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Viral Proteins</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Isatin</term><term>Protease Inhibitors</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Protease Inhibitors</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Chymotrypsin</term><term>Isatin</term><term>Papain</term><term>Protease Inhibitors</term><term>Trypsin</term></keywords><keywords scheme="MESH" qualifier="analogues et dérivés" xml:lang="fr"><term>Isatine</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Protéines virales</term></keywords><keywords scheme="MESH" qualifier="enzymologie" xml:lang="fr"><term>Virus du SRAS</term></keywords><keywords scheme="MESH" qualifier="enzymology" xml:lang="en"><term>SARS Virus</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Chymotrypsine</term><term>Inhibiteurs de protéases</term><term>Isatine</term><term>Papaïne</term><term>Trypsine</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Inhibiteurs de protéases</term><term>Isatine</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Binding Sites</term><term>Computer Simulation</term><term>Cysteine Endopeptidases</term><term>Endopeptidases</term><term>Enzyme Activation</term><term>Fluorescence Resonance Energy Transfer</term><term>Humans</term><term>Molecular Structure</term><term>Structure-Activity Relationship</term><term>Substrate Specificity</term></keywords><keywords scheme="Pascal" xml:lang="fr"><term>Activation enzymatique</term><term>Cysteine endopeptidases</term><term>Endopeptidases</term><term>Humains</term><term>Inhibiteurs de protéases</term><term>Relation structure-activité</term><term>Simulation numérique</term><term>Sites de fixation</term><term>Spécificité du substrat</term><term>Structure moléculaire</term><term>Synthèse chimique</term><term>Isatine</term><term>Transfert d'énergie par résonance de fluorescence</term><term>Virus syndrome respiratoire aigu sévère</term><term>Inhibiteur protease</term><term>Activité biologique</term><term>In vitro</term><term>Sélectivité</term><term>Peptidases</term><term>Antiviral</term><term>Modèle moléculaire</term><term>Complexe enzyme inhibiteur</term><term>Indole dérivé</term><term>Inhibiteur enzyme</term><term>Modélisation</term><term>Indole-2,3-dione(1-[benzo[b]thién-2-ylméthyl]-5-iodo)</term><term>Benzo[b]thiophène dérivé</term><term>benzothiophene</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC<sub>50</sub> values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.</div></front></TEI><affiliations><list><country><li>Taïwan</li></country></list><tree><country name="Taïwan"><noRegion><name sortKey="Chen, Li Rung" sort="Chen, Li Rung" uniqKey="Chen L" first="Li-Rung" last="Chen">Li-Rung Chen</name></noRegion><name sortKey="Chen, Shyh Fong" sort="Chen, Shyh Fong" uniqKey="Chen S" first="Shyh-Fong" last="Chen">Shyh-Fong Chen</name><name sortKey="Chen, Tom Shieh Shung" sort="Chen, Tom Shieh Shung" uniqKey="Chen T" first="Tom Shieh-Shung" last="Chen">Tom Shieh-Shung Chen</name><name sortKey="Chou, Shan Yen" sort="Chou, Shan Yen" uniqKey="Chou S" first="Shan-Yen" last="Chou">Shan-Yen Chou</name><name sortKey="Juang, Shin Hun" sort="Juang, Shin Hun" uniqKey="Juang S" first="Shin-Hun" last="Juang">Shin-Hun Juang</name><name sortKey="Kuo, Chih Jung" sort="Kuo, Chih Jung" uniqKey="Kuo C" first="Chih-Jung" last="Kuo">Chih-Jung Kuo</name><name sortKey="Lee Tai Liu" sort="Lee Tai Liu" uniqKey="Lee Tai Liu" last="Lee Tai Liu">LEE TAI LIU</name><name sortKey="Wang, Yu Chin" sort="Wang, Yu Chin" uniqKey="Wang Y" first="Yu-Chin" last="Wang">Yu-Chin Wang</name><name sortKey="Wu, Ying Ta" sort="Wu, Ying Ta" uniqKey="Wu Y" first="Ying-Ta" last="Wu">Ying-Ta Wu</name><name sortKey="Yi Wen Lin" sort="Yi Wen Lin" uniqKey="Yi Wen Lin" last="Yi Wen Lin">YI WEN LIN</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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