PittsburghV1, PubMed, Checkpoint, bibRecord, 004170

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.

Identifieur interne : 004170 ( PubMed/Checkpoint ); précédent : 004169; suivant : 004171

2-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 [ 1464-3405 ] ; 2014.

RBID : pubmed:25288188

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 (11c) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.

DOI: 10.1016/j.bmcl.2014.09.001
PubMed: 25288188

Affiliations:

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Le document en format XML

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<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>
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<front><div type="abstract" xml:lang="en">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 (11c) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.</div>
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<CopyrightInformation>Copyright © 2014 Elsevier Ltd. All rights reserved.</CopyrightInformation>
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<Initials>MG</Initials>
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<AffiliationInfo><Affiliation>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA.</Affiliation>
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<Author ValidYN="Y"><LastName>Sen</LastName>
<ForeName>Malabika</ForeName>
<Initials>M</Initials>
<AffiliationInfo><Affiliation>Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA.</Affiliation>
</AffiliationInfo>
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<ForeName>Jennifer R</ForeName>
<Initials>JR</Initials>
<AffiliationInfo><Affiliation>Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA; University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA; Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA.</Affiliation>
</AffiliationInfo>
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<Initials>D</Initials>
<AffiliationInfo><Affiliation>Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.</Affiliation>
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<Initials>Y</Initials>
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<ForeName>John S</ForeName>
<Initials>JS</Initials>
<AffiliationInfo><Affiliation>Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA.</Affiliation>
</AffiliationInfo>
</Author>
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<ForeName>Lynn O</ForeName>
<Initials>LO</Initials>
<AffiliationInfo><Affiliation>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA.</Affiliation>
</AffiliationInfo>
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<Initials>P</Initials>
<AffiliationInfo><Affiliation>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA; University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA; Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.</Affiliation>
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<Country>United States</Country>
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<Acronym>CA</Acronym>
<Agency>NCI NIH HHS</Agency>
<Country>United States</Country>
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<Acronym>TR</Acronym>
<Agency>NCATS NIH HHS</Agency>
<Country>United States</Country>
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<Country>United States</Country>
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<Month>09</Month>
<Day>15</Day>
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<MeshHeadingList><MeshHeading><DescriptorName UI="D017209" MajorTopicYN="N">Apoptosis</DescriptorName>
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<MeshHeading><DescriptorName UI="D006801" MajorTopicYN="N">Humans</DescriptorName>
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<MeshHeading><DescriptorName UI="D011485" MajorTopicYN="N">Protein Binding</DescriptorName>
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<QualifierName UI="Q000378" MajorTopicYN="N">metabolism</QualifierName>
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<KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="N">Cancer cell line screening</Keyword>
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<Keyword MajorTopicYN="N">STAT3 pathway</Keyword>
<Keyword MajorTopicYN="N">Skraup synthesis</Keyword>
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<region><li>Pennsylvanie</li>
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<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>
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<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>
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2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.

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