SrasV1, France, Analysis, bibRecord, 000152

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

Identifieur interne : 000152 ( France/Analysis ); précédent : 000151; suivant : 000153

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

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

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

Affiliations:

France, Italie, États-Unis

Links toward previous steps (curation, corpus...)

to stream Hal, to step Corpus: 000119
to stream Hal, to step Curation: 000119
to stream Hal, to step Checkpoint: 000100
to stream Main, to step Merge: 001808
to stream Main, to step Curation: 001802
to stream Main, to step Exploration: 001802
to stream France, to step Extraction: 000152

Links to Exploration step

Hal:pasteur-00968854

Le document en format XML

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            </address>
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</author>
<author><name sortKey="Barresi, Elisabetta" sort="Barresi, Elisabetta" uniqKey="Barresi E" first="Elisabetta" last="Barresi">Elisabetta Barresi</name>
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          <desc>            <address>              <country key="IT"></country>
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<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="Salerno, Silvia" sort="Salerno, Silvia" uniqKey="Salerno S" first="Silvia" last="Salerno">Silvia Salerno</name>
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<country>Italie</country>
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<author><name sortKey="Marchand, Christophe" sort="Marchand, Christophe" uniqKey="Marchand C" first="Christophe" last="Marchand">Christophe Marchand</name>
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</tutelle>
</tutelles>
</hal:affiliation>
<country>États-Unis</country>
</affiliation>
</author>
<author><name sortKey="Agama, Keli" sort="Agama, Keli" uniqKey="Agama K" first="Keli" last="Agama">Keli Agama</name>
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          <desc>            <address>              <addrLine>Center for Cancer Research, Bethesda, Maryland 20892-4255</addrLine>
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          <orgName type="acronym">NCI-NIH</orgName>
          <date type="start">1937-01-01</date>
          <desc>            <address>              <addrLine>BG 9609 MSC 9760, 9609 Medical Center Drive, Bethesda, MD 20892-9760</addrLine>
              <country key="US"></country>
            </address>
            <ref type="url">https://www.cancer.gov/</ref>
          </desc>
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          <orgName type="acronym">NIH</orgName>
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              <country key="US"></country>
            </address>
            <ref type="url">https://www.nih.gov/</ref>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>États-Unis</country>
</affiliation>
</author>
<author><name sortKey="Simorini, Francesca" sort="Simorini, Francesca" uniqKey="Simorini F" first="Francesca" last="Simorini">Francesca Simorini</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-250106" status="INCOMING">          <orgName>Department of Pharmacy</orgName>
          <desc>            <address>              <country key="IT"></country>
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              <country key="IT"></country>
            </address>
            <ref type="url">http://www.unipi.it/index.php/english</ref>
          </desc>
        </org>
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</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="La Motta, Concettina" sort="La Motta, Concettina" uniqKey="La Motta C" first="Concettina" last="La Motta">Concettina La Motta</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-250106" status="INCOMING">          <orgName>Department of Pharmacy</orgName>
          <desc>            <address>              <country key="IT"></country>
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            </address>
            <ref type="url">http://www.unipi.it/index.php/english</ref>
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</tutelle>
</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="Marini, Anna Maria" sort="Marini, Anna Maria" uniqKey="Marini A" first="Anna Maria" last="Marini">Anna Maria Marini</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-250106" status="INCOMING">          <orgName>Department of Pharmacy</orgName>
          <desc>            <address>              <country key="IT"></country>
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            </address>
            <ref type="url">http://www.unipi.it/index.php/english</ref>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="Di Leva, Francesco Saverio" sort="Di Leva, Francesco Saverio" uniqKey="Di Leva F" first="Francesco Saverio" last="Di Leva">Francesco Saverio Di Leva</name>
</author>
<author><name sortKey="Marinelli, Luciana" sort="Marinelli, Luciana" uniqKey="Marinelli L" first="Luciana" last="Marinelli">Luciana Marinelli</name>
</author>
<author><name sortKey="Cosconati, Sandro" sort="Cosconati, Sandro" uniqKey="Cosconati S" first="Sandro" last="Cosconati">Sandro Cosconati</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-190928" status="INCOMING">          <orgName>Department of Pharmaceutical Chemistry and Toxicology</orgName>
          <desc>            <address>              <country key="IT"></country>
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          </desc>
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        <tutelles><tutelle active="#struct-300678" type="direct"><org type="institution" xml:id="struct-300678" status="VALID">          <orgName>Università degli studi di Napoli Federico II</orgName>
          <desc>            <address>              <addrLine>Corso Umberto I 40 - 80138 Napoli</addrLine>
              <country key="IT"></country>
            </address>
            <ref type="url">http://www.unina.it/</ref>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="Novellino, Ettore" sort="Novellino, Ettore" uniqKey="Novellino E" first="Ettore" last="Novellino">Ettore Novellino</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-245682" status="INCOMING">          <orgName>Department of Pharmacy Naples</orgName>
          <desc>            <address>              <addrLine>University of Naples Federico II, via D. Montesano 49, I-80131 Naples</addrLine>
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          <desc>            <address>              <country key="FR"></country>
            </address>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="Pommier, Yves" sort="Pommier, Yves" uniqKey="Pommier Y" first="Yves" last="Pommier">Yves Pommier</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-118139" status="INCOMING">          <orgName>Laboratory of Molecular Pharmacology</orgName>
          <desc>            <address>              <addrLine>National Cancer Institute Bldg. 37, Room 4E28 37 Convent Drive MSC 4255 Bethesda, MD 20892-4255</addrLine>
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<tutelle active="#struct-305678" type="direct"><org type="institution" xml:id="struct-305678" status="VALID">          <orgName>National Cancer Institute [Bethesda]</orgName>
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</hal:affiliation>
<country>France</country>
</affiliation>
</author>
<author><name sortKey="Di Santo, Roberto" sort="Di Santo, Roberto" uniqKey="Di Santo R" first="Roberto" last="Di Santo">Roberto Di Santo</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-251386" status="VALID">          <orgName>Department of Medicinal Chemistry and Technologies</orgName>
          <desc>            <address>              <addrLine>Piazzale Aldo Moro 5, I-00185, Rome</addrLine>
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        <tutelles><tutelle active="#struct-55932" type="direct"><org type="institution" xml:id="struct-55932" status="VALID">          <orgName>Institut Pasteur, Fondation Cenci Bolognetti - Istituto Pasteur Italia, Fondazione Cenci Bolognetti</orgName>
          <desc>            <address>              <addrLine>Université de Rome La Sapienza 5 Place Aldo Moro 00185 Rome</addrLine>
              <country key="IT"></country>
            </address>
            <ref type="url">http://www.istitutopasteur.it/</ref>
          </desc>
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<tutelle active="#struct-301247" type="indirect"><org type="regroupinstitution" xml:id="struct-301247" status="VALID">          <orgName>Réseau International des Instituts Pasteur</orgName>
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          <desc>            <address>              <addrLine>25, rue du Dr Roux 75724 Paris Cedex 15</addrLine>
              <country key="FR"></country>
            </address>
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          </desc>
        </org>
</tutelle>
<tutelle active="#struct-229915" type="direct"><org type="institution" xml:id="struct-229915" status="VALID">          <orgName>Università degli Studi di Roma "La Sapienza" [Rome]</orgName>
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            </address>
            <ref type="url">http://www.uniroma1.it/</ref>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
<author><name sortKey="Da Settimo, Federico" sort="Da Settimo, Federico" uniqKey="Da Settimo F" first="Federico" last="Da Settimo">Federico Da Settimo</name>
<affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-250106" status="INCOMING">          <orgName>Department of Pharmacy</orgName>
          <desc>            <address>              <country key="IT"></country>
            </address>
          </desc>
          <listRelation>            <relation active="#struct-366408" type="direct"></relation>
          </listRelation>
        <tutelles><tutelle active="#struct-366408" type="direct"><org type="institution" xml:id="struct-366408" status="VALID">          <orgName>University of Pisa - Università di Pisa </orgName>
          <desc>            <address>              <addrLine>Lungarno Pacinotti 43 - 56126 Pisa</addrLine>
              <country key="IT"></country>
            </address>
            <ref type="url">http://www.unipi.it/index.php/english</ref>
          </desc>
        </org>
</tutelle>
</tutelles>
</hal:affiliation>
<country>Italie</country>
</affiliation>
</author>
</analytic>
<idno type="DOI">10.1021/jm400932c</idno>
<series><title level="j">Journal of Medicinal Chemistry</title>
<idno type="ISSN">0022-2623</idno>
<imprint><date type="datePub">2013-09-26</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<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>
            </div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
<li>Italie</li>
<li>États-Unis</li>
</country>
</list>
<tree><noCountry><name sortKey="Di Leva, Francesco Saverio" sort="Di Leva, Francesco Saverio" uniqKey="Di Leva F" first="Francesco Saverio" last="Di Leva">Francesco Saverio Di Leva</name>
<name sortKey="Marinelli, Luciana" sort="Marinelli, Luciana" uniqKey="Marinelli L" first="Luciana" last="Marinelli">Luciana Marinelli</name>
</noCountry>
<country name="Italie"><noRegion><name sortKey="Taliani, Sabrina" sort="Taliani, Sabrina" uniqKey="Taliani S" first="Sabrina" last="Taliani">Sabrina Taliani</name>
</noRegion>
<name sortKey="Barresi, Elisabetta" sort="Barresi, Elisabetta" uniqKey="Barresi E" first="Elisabetta" last="Barresi">Elisabetta Barresi</name>
<name sortKey="Cosconati, Sandro" sort="Cosconati, Sandro" uniqKey="Cosconati S" first="Sandro" last="Cosconati">Sandro Cosconati</name>
<name sortKey="Da Settimo, Federico" sort="Da Settimo, Federico" uniqKey="Da Settimo F" first="Federico" last="Da Settimo">Federico Da Settimo</name>
<name sortKey="Di Santo, Roberto" sort="Di Santo, Roberto" uniqKey="Di Santo R" first="Roberto" last="Di Santo">Roberto Di Santo</name>
<name sortKey="La Motta, Concettina" sort="La Motta, Concettina" uniqKey="La Motta C" first="Concettina" last="La Motta">Concettina La Motta</name>
<name sortKey="Marini, Anna Maria" sort="Marini, Anna Maria" uniqKey="Marini A" first="Anna Maria" last="Marini">Anna Maria Marini</name>
<name sortKey="Novellino, Ettore" sort="Novellino, Ettore" uniqKey="Novellino E" first="Ettore" last="Novellino">Ettore Novellino</name>
<name sortKey="Pugliesi, Isabella" sort="Pugliesi, Isabella" uniqKey="Pugliesi I" first="Isabella" last="Pugliesi">Isabella Pugliesi</name>
<name sortKey="Salerno, Silvia" sort="Salerno, Silvia" uniqKey="Salerno S" first="Silvia" last="Salerno">Silvia Salerno</name>
<name sortKey="Simorini, Francesca" sort="Simorini, Francesca" uniqKey="Simorini F" first="Francesca" last="Simorini">Francesca Simorini</name>
</country>
<country name="États-Unis"><noRegion><name sortKey="Marchand, Christophe" sort="Marchand, Christophe" uniqKey="Marchand C" first="Christophe" last="Marchand">Christophe Marchand</name>
</noRegion>
<name sortKey="Agama, Keli" sort="Agama, Keli" uniqKey="Agama K" first="Keli" last="Agama">Keli Agama</name>
</country>
<country name="France"><noRegion><name sortKey="Pommier, Yves" sort="Pommier, Yves" uniqKey="Pommier Y" first="Yves" last="Pommier">Yves Pommier</name>
</noRegion>
</country>
</tree>
</affiliations>
</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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