SrasV1, Hal, Corpus, bibRecord, 000119

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

Identifieur interne : 000119 ( Hal/Corpus ); précédent : 000118; suivant : 000120

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

Auteurs : Sabrina Taliani ; Isabella Pugliesi ; Elisabetta Barresi ; Silvia Salerno ; Christophe Marchand ; Keli Agama ; Francesca Simorini ; Concettina La Motta ; Anna Maria Marini ; Francesco Saverio Di Leva ; Luciana Marinelli ; Sandro Cosconati ; Ettore Novellino ; Yves Pommier ; Roberto Di Santo ; Federico Da Settimo

Source :

Journal of Medicinal Chemistry [ 0022-2623 ] ; 2013-09-26.

RBID : Hal:pasteur-00968854

Abstract

In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted phenyl ring at 2- or 3-position, a protonable side chain at 4- or 5-position), affording a number of Top1 inhibitors with cleavage patterns common to CPT and MJ-III-65. SARs data were rationalized by means of an advanced docking protocol.

Url:

https://hal-riip.archives-ouvertes.fr/pasteur-00968854

DOI: 10.1021/jm400932c

Links to Exploration step

Hal:pasteur-00968854

Le document en format XML

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<idno type="DOI">10.1021/jm400932c</idno>
<series><title level="j">Journal of Medicinal Chemistry</title>
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<front><div type="abstract" xml:lang="en">              <p>In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted phenyl ring at 2- or 3-position, a protonable side chain at 4- or 5-position), affording a number of Top1 inhibitors with cleavage patterns common to CPT and MJ-III-65. SARs data were rationalized by means of an advanced docking protocol.</p>
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                  <email type="domain">farm.unipi.it</email>
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                <author role="aut">                  <persName>                    <forename type="first">Isabella</forename>
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                <author role="aut">                  <persName>                    <forename type="first">Elisabetta</forename>
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                <author role="aut">                  <persName>                    <forename type="first">Francesca</forename>
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                  <affiliation ref="#struct-250106"></affiliation>
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                    <surname>Novellino</surname>
                  </persName>
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                  <affiliation ref="#struct-245682"></affiliation>
                </author>
                <author role="aut">                  <persName>                    <forename type="first">Yves</forename>
                    <surname>Pommier</surname>
                  </persName>
                  <idno type="halauthorid">140137</idno>
                  <affiliation ref="#struct-118139"></affiliation>
                </author>
                <author role="aut">                  <persName>                    <forename type="first">Roberto</forename>
                    <surname>Di Santo</surname>
                  </persName>
                  <idno type="halauthorid">1006363</idno>
                  <affiliation ref="#struct-251386"></affiliation>
                </author>
                <author role="aut">                  <persName>                    <forename type="first">Federico</forename>
                    <surname>Da Settimo</surname>
                  </persName>
                  <idno type="halauthorid">719843</idno>
                  <affiliation ref="#struct-250106"></affiliation>
                </author>
              </analytic>
              <monogr>                <idno type="halJournalId" status="VALID">15785</idno>
                <idno type="issn">0022-2623</idno>
                <idno type="eissn">1520-4804</idno>
                <title level="j">Journal of Medicinal Chemistry</title>
                <imprint>                  <publisher>American Chemical Society</publisher>
                  <biblScope unit="volume">56</biblScope>
                  <biblScope unit="issue">18</biblScope>
                  <biblScope unit="pp">7458-62</biblScope>
                  <date type="datePub">2013-09-26</date>
                  <date type="dateEpub">2013-09-16</date>
                </imprint>
              </monogr>
              <idno type="doi">10.1021/jm400932c</idno>
              <idno type="pubmed">23987476</idno>
            </biblStruct>
          </sourceDesc>
          <profileDesc>            <langUsage>              <language ident="en">English</language>
            </langUsage>
            <textClass>              <classCode scheme="mesh">Drug Discovery</classCode>
              <classCode scheme="mesh">Heterocyclic Compounds, 3-Ring</classCode>
              <classCode scheme="mesh">Humans</classCode>
              <classCode scheme="mesh">Molecular Docking Simulation</classCode>
              <classCode scheme="mesh">Protein Conformation</classCode>
              <classCode scheme="mesh">Pyrroles</classCode>
              <classCode scheme="mesh">Quinazolines</classCode>
              <classCode scheme="mesh">Topoisomerase I Inhibitors</classCode>
              <classCode scheme="mesh">DNA Topoisomerases, Type I</classCode>
              <classCode scheme="halDomain" n="sdv.sp">Life Sciences [q-bio]/Pharmaceutical sciences</classCode>
              <classCode scheme="halTypology" n="ART">Journal articles</classCode>
            </textClass>
            <abstract xml:lang="en">              <p>In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted phenyl ring at 2- or 3-position, a protonable side chain at 4- or 5-position), affording a number of Top1 inhibitors with cleavage patterns common to CPT and MJ-III-65. SARs data were rationalized by means of an advanced docking protocol.</p>
            </abstract>
          </profileDesc>
        </hal>
</record>

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Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

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