Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.
Identifieur interne : 000323 ( Hal/Curation ); précédent : 000322; suivant : 000324Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.
Auteurs : Yoann Joyard ; Vadim Le Joncour [France] ; Hélène Castel ; Chérif Bounana Diouf ; Laurent Bischoff [France] ; Cyril Papamicaël [France] ; Vincent Levacher [France] ; Pierre Vera [France] ; Pierre Bohn [France]Source :
Abstract
Tumor hypoxia plays a major role in reducing the efficacy of therapeutic modalities like chemotherapy and radiation therapy in combating cancer. In order to target hypoxic tissues, a tripeptide ligand having a 2-nitroimidazole moiety, as a bioreductive species, was synthesized. The latter was radiolabeled with (99m)Tc for imaging hypoxic regions of tumors and was characterized by means of its rhenium analogue. The biodistribution and scintigraphic image of the corresponding (99m)Tc-complex showed accumulation in tumor and these results suggest that it could be a marker for imaging tumor hypoxia.
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DOI: 10.1016/j.bmcl.2013.05.015
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In order to target hypoxic tissues, a tripeptide ligand having a 2-nitroimidazole moiety, as a bioreductive species, was synthesized. The latter was radiolabeled with (99m)Tc for imaging hypoxic regions of tumors and was characterized by means of its rhenium analogue. The biodistribution and scintigraphic image of the corresponding (99m)Tc-complex showed accumulation in tumor and these results suggest that it could be a marker for imaging tumor hypoxia.</div></front></TEI><hal api="V3"><titleStmt><title xml:lang="en">Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.</title><author role="aut"><persName><forename type="first">Yoann</forename><surname>Joyard</surname></persName><email></email><idno type="halauthor">975897</idno></author><author role="aut"><persName><forename type="first">Vadim</forename><surname>Le Joncour</surname></persName><email></email><idno type="halauthor">776958</idno><affiliation ref="#struct-106121"></affiliation></author><author role="aut"><persName><forename type="first">Hélène</forename><surname>Castel</surname></persName><email></email><idno type="halauthor">1026995</idno></author><author role="aut"><persName><forename type="first">Chérif Bounana</forename><surname>Diouf</surname></persName><email></email><idno type="halauthor">1027698</idno></author><author role="aut"><persName><forename type="first">Laurent</forename><surname>Bischoff</surname></persName><email></email><idno type="halauthor">475782</idno><affiliation ref="#struct-141329"></affiliation></author><author role="aut"><persName><forename type="first">Cyril</forename><surname>Papamicaël</surname></persName><email></email><idno type="halauthor">475833</idno><affiliation ref="#struct-797"></affiliation></author><author role="aut"><persName><forename type="first">Vincent</forename><surname>Levacher</surname></persName><email></email><idno type="halauthor">475815</idno><affiliation ref="#struct-141329"></affiliation></author><author role="aut"><persName><forename type="first">Pierre</forename><surname>Vera</surname></persName><email></email><idno type="halauthor">348291</idno><affiliation ref="#struct-23832"></affiliation><affiliation ref="#struct-110210"></affiliation></author><author role="aut"><persName><forename type="first">Pierre</forename><surname>Bohn</surname></persName><email></email><idno type="halauthor">475777</idno><affiliation ref="#struct-23832"></affiliation><affiliation ref="#struct-110210"></affiliation></author><editor role="depositor"><persName><forename>Umr 6014</forename><surname>Cobra</surname></persName><email>dir-cobra@insa-rouen.fr</email></editor></titleStmt><editionStmt><edition n="v1" type="current"><date type="whenSubmitted">2014-05-28 10:35:54</date><date type="whenModified">2015-12-04 12:13:19</date><date type="whenReleased">2014-05-28 10:35:53</date><date type="whenProduced">2013-07-01</date></edition><respStmt><resp>contributor</resp><name key="195158"><persName><forename>Umr 6014</forename><surname>Cobra</surname></persName><email>dir-cobra@insa-rouen.fr</email></name></respStmt></editionStmt><publicationStmt><distributor>CCSD</distributor><idno type="halId">hal-00997430</idno><idno type="halUri">https://hal.archives-ouvertes.fr/hal-00997430</idno><idno type="halBibtex">joyard:hal-00997430</idno><idno type="halRefHtml">Bioorganic & Medicinal Chemistry Letters, Elsevier, 2013, 23 (13), pp.3704-8. <10.1016/j.bmcl.2013.05.015></idno><idno type="halRef">Bioorganic & Medicinal Chemistry Letters, Elsevier, 2013, 23 (13), pp.3704-8. <10.1016/j.bmcl.2013.05.015></idno></publicationStmt><seriesStmt><idno type="stamp" n="CNRS">CNRS - Centre national de la recherche scientifique</idno><idno type="stamp" n="UNIV-LEHAVRE">Université du Havre</idno><idno type="stamp" n="UNIV-ROUEN">Université de Rouen</idno><idno type="stamp" n="LITIS">Laboratoire d'Informatique, de Traitement de l'Information et des Systèmes</idno><idno type="stamp" n="FNCLCC" p="INSERM">UNICANCER</idno><idno type="stamp" n="BECQUEREL" p="INSERM">Centre Henri Becquerel</idno><idno type="stamp" n="COMUE-NORMANDIE">Normandie Université</idno><idno type="stamp" n="INC-CNRS">Institut de Chimie du CNRS</idno></seriesStmt><notesStmt><note type="audience" n="2">International</note><note type="popular" n="0">No</note><note type="peer" n="1">Yes</note></notesStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.</title><author role="aut"><persName><forename type="first">Yoann</forename><surname>Joyard</surname></persName><idno type="halAuthorId">975897</idno></author><author role="aut"><persName><forename type="first">Vadim</forename><surname>Le Joncour</surname></persName><idno type="halAuthorId">776958</idno><affiliation ref="#struct-106121"></affiliation></author><author role="aut"><persName><forename type="first">Hélène</forename><surname>Castel</surname></persName><idno type="halAuthorId">1026995</idno></author><author role="aut"><persName><forename type="first">Chérif Bounana</forename><surname>Diouf</surname></persName><idno type="halAuthorId">1027698</idno></author><author role="aut"><persName><forename type="first">Laurent</forename><surname>Bischoff</surname></persName><idno type="halAuthorId">475782</idno><affiliation ref="#struct-141329"></affiliation></author><author role="aut"><persName><forename type="first">Cyril</forename><surname>Papamicaël</surname></persName><idno type="halAuthorId">475833</idno><affiliation ref="#struct-797"></affiliation></author><author role="aut"><persName><forename type="first">Vincent</forename><surname>Levacher</surname></persName><idno type="halAuthorId">475815</idno><affiliation ref="#struct-141329"></affiliation></author><author role="aut"><persName><forename type="first">Pierre</forename><surname>Vera</surname></persName><idno type="halAuthorId">348291</idno><affiliation ref="#struct-23832"></affiliation><affiliation ref="#struct-110210"></affiliation></author><author role="aut"><persName><forename type="first">Pierre</forename><surname>Bohn</surname></persName><idno type="halAuthorId">475777</idno><affiliation ref="#struct-23832"></affiliation><affiliation ref="#struct-110210"></affiliation></author></analytic><monogr><idno type="halJournalId" status="VALID">110449</idno><title level="j">Bioorganic & Medicinal Chemistry Letters</title><imprint><publisher>Elsevier</publisher><biblScope unit="volume">23</biblScope><biblScope unit="issue">13</biblScope><biblScope unit="pp">3704-8</biblScope><date type="datePub">2013-07-01</date></imprint></monogr><idno type="doi">10.1016/j.bmcl.2013.05.015</idno><idno type="pubmed">23726027</idno></biblStruct></sourceDesc><profileDesc><langUsage><language ident="en">English</language></langUsage><textClass><classCode scheme="halDomain" n="chim.orga">Chemical Sciences/Organic chemistry</classCode><classCode scheme="halTypology" n="ART">Journal articles</classCode></textClass><abstract xml:lang="en">Tumor hypoxia plays a major role in reducing the efficacy of therapeutic modalities like chemotherapy and radiation therapy in combating cancer. In order to target hypoxic tissues, a tripeptide ligand having a 2-nitroimidazole moiety, as a bioreductive species, was synthesized. The latter was radiolabeled with (99m)Tc for imaging hypoxic regions of tumors and was characterized by means of its rhenium analogue. The biodistribution and scintigraphic image of the corresponding (99m)Tc-complex showed accumulation in tumor and these results suggest that it could be a marker for imaging tumor hypoxia.</abstract></profileDesc></hal></record>Pour manipuler ce document sous Unix (Dilib)
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