2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway
Identifieur interne : 004489 ( Main/Exploration ); précédent : 004488; suivant : 0044902-Guanidinoquinazolines as new inhibitors of the STAT3 pathway
Auteurs : Matthew G. Laporte [États-Unis] ; Dimas José Da Paz Lima [États-Unis] ; Feng Zhang [États-Unis] ; Malabika Sen [États-Unis] ; Jennifer R. Grandis [États-Unis] ; Daniel Camarco [États-Unis] ; Yun Hua [États-Unis] ; Paul A. Johnston [États-Unis] ; John S. Lazo [États-Unis] ; Lynn O. Resnick [États-Unis] ; Peter Wipf [États-Unis] ; Donna M. Huryn [États-Unis]Source :
- Bioorganic & medicinal chemistry letters [ 0960-894X ] ; 2014.
Descripteurs français
- KwdFr :
- Apoptose (), Facteur de transcription STAT-3 (antagonistes et inhibiteurs), Facteur de transcription STAT-3 (métabolisme), Guanidine (), Humains, Liaison aux protéines, Lignée cellulaire tumorale, Prolifération cellulaire (), Quinazolines (), Quinazolines (métabolisme), Quinazolines (toxicité), Relation structure-activité.
- MESH :
- antagonistes et inhibiteurs : Facteur de transcription STAT-3.
- métabolisme : Facteur de transcription STAT-3, Quinazolines.
- toxicité : Quinazolines.
- Apoptose, Guanidine, Humains, Liaison aux protéines, Lignée cellulaire tumorale, Prolifération cellulaire, Quinazolines, Relation structure-activité.
English descriptors
- KwdEn :
- Apoptosis (drug effects), Cell Line, Tumor, Cell Proliferation (drug effects), Guanidine (chemistry), Humans, Protein Binding, Quinazolines (chemistry), Quinazolines (metabolism), Quinazolines (toxicity), STAT3 Transcription Factor (antagonists & inhibitors), STAT3 Transcription Factor (metabolism), Structure-Activity Relationship.
- MESH :
- chemical , antagonists & inhibitors : STAT3 Transcription Factor.
- chemical , chemistry : Guanidine, Quinazolines.
- drug effects : Apoptosis, Cell Proliferation.
- chemical , metabolism : Quinazolines, STAT3 Transcription Factor.
- chemical , toxicity : Quinazolines.
- Cell Line, Tumor, Humans, Protein Binding, Structure-Activity Relationship.
Abstract
Synthesis and SAR investigation of 2-guanidinoquinazolines, initially identified in a high content screen for selective STAT3 pathway inhibitors, led to a more potent analog (
Url:
DOI: 10.1016/j.bmcl.2014.09.001
PubMed: 25288188
PubMed Central: 4250329
Affiliations:
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Le document en format XML
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Laporte</name><affiliation wicri:level="2"><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName></affiliation></author><author><name sortKey="Da Paz Lima, Dimas Jose" sort="Da Paz Lima, Dimas Jose" uniqKey="Da Paz Lima D" first="Dimas José" last="Da Paz Lima">Dimas José Da Paz Lima</name><affiliation wicri:level="2"><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName></affiliation></author><author><name sortKey="Zhang, Feng" sort="Zhang, Feng" uniqKey="Zhang F" first="Feng" last="Zhang">Feng Zhang</name><affiliation wicri:level="2"><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName></affiliation></author><author><name sortKey="Sen, Malabika" sort="Sen, Malabika" uniqKey="Sen M" first="Malabika" last="Sen">Malabika Sen</name><affiliation wicri:level="4"><nlm:aff id="A2">Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName></affiliation></author><author><name sortKey="Grandis, Jennifer R" sort="Grandis, Jennifer R" uniqKey="Grandis J" first="Jennifer R." last="Grandis">Jennifer R. Grandis</name><affiliation wicri:level="4"><nlm:aff id="A2">Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName></affiliation><affiliation wicri:level="2"><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName></affiliation><affiliation wicri:level="4"><nlm:aff id="A4">Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName></affiliation></author><author><name sortKey="Camarco, Daniel" sort="Camarco, Daniel" uniqKey="Camarco D" first="Daniel" last="Camarco">Daniel Camarco</name><affiliation wicri:level="4"><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName></affiliation></author><author><name sortKey="Hua, Yun" sort="Hua, Yun" uniqKey="Hua Y" first="Yun" last="Hua">Yun Hua</name><affiliation wicri:level="4"><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName></affiliation></author><author><name sortKey="Johnston, Paul A" sort="Johnston, Paul A" uniqKey="Johnston P" first="Paul A." last="Johnston">Paul A. 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Lazo</name><affiliation wicri:level="2"><nlm:aff id="A6">Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmacology, University of Virginia, Charlottesville, VA 22908</wicri:regionArea><placeName><region type="state">Virginie</region></placeName></affiliation></author><author><name sortKey="Resnick, Lynn O" sort="Resnick, Lynn O" uniqKey="Resnick L" first="Lynn O." last="Resnick">Lynn O. Resnick</name><affiliation wicri:level="2"><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName></affiliation></author><author><name sortKey="Wipf, Peter" sort="Wipf, Peter" uniqKey="Wipf P" first="Peter" last="Wipf">Peter Wipf</name><affiliation wicri:level="2"><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName><placeName><settlement type="city">Pittsburgh</settlement><region type="state">Pennsylvanie</region></placeName><orgName type="university" n="3">Université de Pittsburgh</orgName></affiliation><affiliation wicri:level="2"><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName><placeName><settlement type="city">Pittsburgh</settlement><region type="state">Pennsylvanie</region></placeName><orgName type="university" n="3">Université de Pittsburgh</orgName></affiliation><affiliation wicri:level="4"><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName><placeName><settlement type="city">Pittsburgh</settlement><region type="state">Pennsylvanie</region></placeName><orgName type="university" n="3">Université de Pittsburgh</orgName></affiliation></author><author><name sortKey="Huryn, Donna M" sort="Huryn, Donna M" uniqKey="Huryn D" first="Donna M." last="Huryn">Donna M. Huryn</name><affiliation wicri:level="2"><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region></placeName></affiliation><affiliation wicri:level="4"><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260</wicri:regionArea><placeName><region type="state">Pennsylvanie</region><settlement type="city">Pittsburgh</settlement></placeName><orgName type="university">Université de Pittsburgh</orgName></affiliation></author></analytic><series><title level="j">Bioorganic & medicinal chemistry letters</title><idno type="ISSN">0960-894X</idno><idno type="eISSN">1464-3405</idno><imprint><date when="2014">2014</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Apoptosis (drug effects)</term><term>Cell Line, Tumor</term><term>Cell Proliferation (drug effects)</term><term>Guanidine (chemistry)</term><term>Humans</term><term>Protein Binding</term><term>Quinazolines (chemistry)</term><term>Quinazolines (metabolism)</term><term>Quinazolines (toxicity)</term><term>STAT3 Transcription Factor (antagonists & inhibitors)</term><term>STAT3 Transcription Factor (metabolism)</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Apoptose ()</term><term>Facteur de transcription STAT-3 (antagonistes et inhibiteurs)</term><term>Facteur de transcription STAT-3 (métabolisme)</term><term>Guanidine ()</term><term>Humains</term><term>Liaison aux protéines</term><term>Lignée cellulaire tumorale</term><term>Prolifération cellulaire ()</term><term>Quinazolines ()</term><term>Quinazolines (métabolisme)</term><term>Quinazolines (toxicité)</term><term>Relation structure-activité</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>STAT3 Transcription Factor</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Guanidine</term><term>Quinazolines</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Facteur de transcription STAT-3</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Apoptosis</term><term>Cell Proliferation</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Quinazolines</term><term>STAT3 Transcription Factor</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Facteur de transcription STAT-3</term><term>Quinazolines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="toxicity" xml:lang="en"><term>Quinazolines</term></keywords><keywords scheme="MESH" qualifier="toxicité" xml:lang="fr"><term>Quinazolines</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Cell Line, Tumor</term><term>Humans</term><term>Protein Binding</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Apoptose</term><term>Guanidine</term><term>Humains</term><term>Liaison aux protéines</term><term>Lignée cellulaire tumorale</term><term>Prolifération cellulaire</term><term>Quinazolines</term><term>Relation structure-activité</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><p id="P1">Synthesis and SAR investigation of 2-guanidinoquinazolines, initially identified in a high content screen for selective STAT3 pathway inhibitors, led to a more potent analog (<bold>11c</bold>) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.</p></div></front></TEI><affiliations><list><country><li>États-Unis</li></country><region><li>Pennsylvanie</li><li>Virginie</li></region><settlement><li>Pittsburgh</li></settlement><orgName><li>Université de Pittsburgh</li></orgName></list><tree><country name="États-Unis"><region name="Pennsylvanie"><name sortKey="Laporte, Matthew G" sort="Laporte, Matthew G" uniqKey="Laporte M" first="Matthew G." last="Laporte">Matthew G. Laporte</name></region><name sortKey="Camarco, Daniel" sort="Camarco, Daniel" uniqKey="Camarco D" first="Daniel" last="Camarco">Daniel Camarco</name><name sortKey="Da Paz Lima, Dimas Jose" sort="Da Paz Lima, Dimas Jose" uniqKey="Da Paz Lima D" first="Dimas José" last="Da Paz Lima">Dimas José Da Paz Lima</name><name sortKey="Grandis, Jennifer R" sort="Grandis, Jennifer R" uniqKey="Grandis J" first="Jennifer R." last="Grandis">Jennifer R. Grandis</name><name sortKey="Grandis, Jennifer R" sort="Grandis, Jennifer R" uniqKey="Grandis J" first="Jennifer R." last="Grandis">Jennifer R. Grandis</name><name sortKey="Grandis, Jennifer R" sort="Grandis, Jennifer R" uniqKey="Grandis J" first="Jennifer R." last="Grandis">Jennifer R. Grandis</name><name sortKey="Hua, Yun" sort="Hua, Yun" uniqKey="Hua Y" first="Yun" last="Hua">Yun Hua</name><name sortKey="Huryn, Donna M" sort="Huryn, Donna M" uniqKey="Huryn D" first="Donna M." last="Huryn">Donna M. Huryn</name><name sortKey="Huryn, Donna M" sort="Huryn, Donna M" uniqKey="Huryn D" first="Donna M." last="Huryn">Donna M. Huryn</name><name sortKey="Johnston, Paul A" sort="Johnston, Paul A" uniqKey="Johnston P" first="Paul A." last="Johnston">Paul A. Johnston</name><name sortKey="Johnston, Paul A" sort="Johnston, Paul A" uniqKey="Johnston P" first="Paul A." last="Johnston">Paul A. Johnston</name><name sortKey="Lazo, John S" sort="Lazo, John S" uniqKey="Lazo J" first="John S." last="Lazo">John S. Lazo</name><name sortKey="Resnick, Lynn O" sort="Resnick, Lynn O" uniqKey="Resnick L" first="Lynn O." last="Resnick">Lynn O. Resnick</name><name sortKey="Sen, Malabika" sort="Sen, Malabika" uniqKey="Sen M" first="Malabika" last="Sen">Malabika Sen</name><name sortKey="Wipf, Peter" sort="Wipf, Peter" uniqKey="Wipf P" first="Peter" last="Wipf">Peter Wipf</name><name sortKey="Wipf, Peter" sort="Wipf, Peter" uniqKey="Wipf P" first="Peter" last="Wipf">Peter Wipf</name><name sortKey="Wipf, Peter" sort="Wipf, Peter" uniqKey="Wipf P" first="Peter" last="Wipf">Peter Wipf</name><name sortKey="Zhang, Feng" sort="Zhang, Feng" uniqKey="Zhang F" first="Feng" last="Zhang">Feng Zhang</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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