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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway</title><author><name sortKey="Laporte, Matthew G" sort="Laporte, Matthew G" uniqKey="Laporte M" first="Matthew G." last="Laporte">Matthew G. Laporte</name><affiliation><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Zhang, Feng" sort="Zhang, Feng" uniqKey="Zhang F" first="Feng" last="Zhang">Feng Zhang</name><affiliation><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Sen, Malabika" sort="Sen, Malabika" uniqKey="Sen M" first="Malabika" last="Sen">Malabika Sen</name><affiliation><nlm:aff id="A2">Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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><nlm:aff id="A2">Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A4">Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Camarco, Daniel" sort="Camarco, Daniel" uniqKey="Camarco D" first="Daniel" last="Camarco">Daniel Camarco</name><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Hua, Yun" sort="Hua, Yun" uniqKey="Hua Y" first="Yun" last="Hua">Yun Hua</name><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Johnston, Paul A" sort="Johnston, Paul A" uniqKey="Johnston P" first="Paul A." last="Johnston">Paul A. Johnston</name><affiliation><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Lazo, John S" sort="Lazo, John S" uniqKey="Lazo J" first="John S." last="Lazo">John S. Lazo</name><affiliation><nlm:aff id="A6">Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA</nlm:aff></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><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Wipf, Peter" sort="Wipf, Peter" uniqKey="Wipf P" first="Peter" last="Wipf">Peter Wipf</name><affiliation><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PMC</idno><idno type="pmid">25288188</idno><idno type="pmc">4250329</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4250329</idno><idno type="RBID">PMC:4250329</idno><idno type="doi">10.1016/j.bmcl.2014.09.001</idno><date when="2014">2014</date><idno type="wicri:Area/Pmc/Corpus">001763</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">001763</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway</title><author><name sortKey="Laporte, Matthew G" sort="Laporte, Matthew G" uniqKey="Laporte M" first="Matthew G." last="Laporte">Matthew G. Laporte</name><affiliation><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Zhang, Feng" sort="Zhang, Feng" uniqKey="Zhang F" first="Feng" last="Zhang">Feng Zhang</name><affiliation><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Sen, Malabika" sort="Sen, Malabika" uniqKey="Sen M" first="Malabika" last="Sen">Malabika Sen</name><affiliation><nlm:aff id="A2">Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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><nlm:aff id="A2">Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A4">Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Camarco, Daniel" sort="Camarco, Daniel" uniqKey="Camarco D" first="Daniel" last="Camarco">Daniel Camarco</name><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Hua, Yun" sort="Hua, Yun" uniqKey="Hua Y" first="Yun" last="Hua">Yun Hua</name><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Johnston, Paul A" sort="Johnston, Paul A" uniqKey="Johnston P" first="Paul A." last="Johnston">Paul A. Johnston</name><affiliation><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Lazo, John S" sort="Lazo, John S" uniqKey="Lazo J" first="John S." last="Lazo">John S. Lazo</name><affiliation><nlm:aff id="A6">Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA</nlm:aff></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><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation></author><author><name sortKey="Wipf, Peter" sort="Wipf, Peter" uniqKey="Wipf P" first="Peter" last="Wipf">Peter Wipf</name><affiliation><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A3">University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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><nlm:aff id="A1">University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></affiliation><affiliation><nlm:aff id="A5">Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</nlm:aff></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></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><pmc article-type="research-article"><pmc-comment>The publisher of this article does not allow downloading of the full text in XML form.</pmc-comment>
<pmc-dir>properties manuscript</pmc-dir>
<front><journal-meta><journal-id journal-id-type="nlm-journal-id">9107377</journal-id><journal-id journal-id-type="pubmed-jr-id">20409</journal-id><journal-id journal-id-type="nlm-ta">Bioorg Med Chem Lett</journal-id><journal-id journal-id-type="iso-abbrev">Bioorg. Med. Chem. Lett.</journal-id><journal-title-group><journal-title>Bioorganic & medicinal chemistry letters</journal-title></journal-title-group><issn pub-type="ppub">0960-894X</issn><issn pub-type="epub">1464-3405</issn></journal-meta><article-meta><article-id pub-id-type="pmid">25288188</article-id><article-id pub-id-type="pmc">4250329</article-id><article-id pub-id-type="doi">10.1016/j.bmcl.2014.09.001</article-id><article-id pub-id-type="manuscript">NIHMS627747</article-id><article-categories><subj-group subj-group-type="heading"><subject>Article</subject></subj-group></article-categories><title-group><article-title>2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway</article-title></title-group><contrib-group><contrib contrib-type="author"><name><surname>LaPorte</surname><given-names>Matthew G.</given-names></name><xref ref-type="aff" rid="A1">a</xref><xref ref-type="corresp" rid="CR1">*</xref></contrib><contrib contrib-type="author"><name><surname>da Paz Lima</surname><given-names>Dimas José</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Zhang</surname><given-names>Feng</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Sen</surname><given-names>Malabika</given-names></name><xref ref-type="aff" rid="A2">b</xref></contrib><contrib contrib-type="author"><name><surname>Grandis</surname><given-names>Jennifer R.</given-names></name><xref ref-type="aff" rid="A2">b</xref><xref ref-type="aff" rid="A3">c</xref><xref ref-type="aff" rid="A4">d</xref></contrib><contrib contrib-type="author"><name><surname>Camarco</surname><given-names>Daniel</given-names></name><xref ref-type="aff" rid="A5">e</xref></contrib><contrib contrib-type="author"><name><surname>Hua</surname><given-names>Yun</given-names></name><xref ref-type="aff" rid="A5">e</xref></contrib><contrib contrib-type="author"><name><surname>Johnston</surname><given-names>Paul A.</given-names></name><xref ref-type="aff" rid="A3">c</xref><xref ref-type="aff" rid="A5">e</xref></contrib><contrib contrib-type="author"><name><surname>Lazo</surname><given-names>John S.</given-names></name><xref ref-type="aff" rid="A6">f</xref></contrib><contrib contrib-type="author"><name><surname>Resnick</surname><given-names>Lynn O.</given-names></name><xref ref-type="aff" rid="A1">a</xref></contrib><contrib contrib-type="author"><name><surname>Wipf</surname><given-names>Peter</given-names></name><xref ref-type="aff" rid="A1">a</xref><xref ref-type="aff" rid="A3">c</xref><xref ref-type="aff" rid="A5">e</xref></contrib><contrib contrib-type="author"><name><surname>Huryn</surname><given-names>Donna M.</given-names></name><xref ref-type="aff" rid="A1">a</xref><xref ref-type="aff" rid="A5">e</xref><xref ref-type="corresp" rid="CR1">*</xref></contrib></contrib-group><aff id="A1"><label>a</label>University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA</aff><aff id="A2"><label>b</label>Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA</aff><aff id="A3"><label>c</label>University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA</aff><aff id="A4"><label>d</label>Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA</aff><aff id="A5"><label>e</label>Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA</aff><aff id="A6"><label>f</label>Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA</aff><author-notes><corresp id="CR1"><label>*</label>Corresponding authors. Tel.: +1 412 624 8004 (M.G.L.), +1 412 737 3225 (D.M.H.). <email>mgl12@pitt.edu</email> (M.G. LaPorte), <email>huryn@pitt.edu</email> (D.M. Huryn).</corresp></author-notes><pub-date pub-type="nihms-submitted"><day>10</day><month>10</month><year>2014</year></pub-date><pub-date pub-type="epub"><day>15</day><month>9</month><year>2014</year></pub-date><pub-date pub-type="ppub"><day>1</day><month>11</month><year>2014</year></pub-date><pub-date pub-type="pmc-release"><day>01</day><month>11</month><year>2015</year></pub-date><volume>24</volume><issue>21</issue><fpage>5081</fpage><lpage>5085</lpage><pmc-comment>elocation-id from pubmed: 10.1016/j.bmcl.2014.09.001</pmc-comment>
<permissions><copyright-statement>© 2014 Elsevier Ltd. All rights reserved.</copyright-statement><copyright-year>2014</copyright-year></permissions><abstract><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></abstract><kwd-group><kwd>STAT3 pathway</kwd><kwd>Guanidinoquinazolines</kwd><kwd>Skraup synthesis</kwd><kwd>Structure–activity relationships</kwd><kwd>Cancer cell line screening</kwd></kwd-group></article-meta></front></pmc></record>Pour manipuler ce document sous Unix (Dilib)
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