Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.
Identifieur interne : 000412 ( Main/Exploration ); précédent : 000411; suivant : 000413Synthesis 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.
Url:
DOI: 10.1016/j.bmcl.2013.05.015
Affiliations:
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76821 - Mont Saint Aignan</addrLine><country key="FR"></country></address></desc><listRelation><relation active="#struct-301288" type="direct"></relation><relation active="#struct-301232" type="indirect"></relation><relation name="UMR6014" active="#struct-441569" type="direct"></relation></listRelation><tutelles><tutelle active="#struct-301288" type="direct"><org type="department" xml:id="struct-301288" status="VALID"><orgName>Institut National des Sciences Appliquées - Rouen</orgName><orgName type="acronym">INSA Rouen</orgName><desc><address><country key="FR"></country></address></desc><listRelation><relation active="#struct-301232" type="direct"></relation></listRelation></org></tutelle><tutelle active="#struct-301232" type="indirect"><org type="institution" xml:id="struct-301232" status="VALID"><orgName>Institut National des Sciences Appliquées</orgName><orgName type="acronym">INSA</orgName><desc><address><country key="FR"></country></address></desc></org></tutelle><tutelle name="UMR6014" active="#struct-441569" type="direct"><org type="institution" xml:id="struct-441569" status="VALID"><idno type="ISNI">0000000122597504</idno><idno type="IdRef">02636817X</idno><orgName>Centre National de la Recherche Scientifique</orgName><orgName type="acronym">CNRS</orgName><date type="start">1939-10-19</date><desc><address><country key="FR"></country></address><ref type="url">http://www.cnrs.fr/</ref></desc></org></tutelle></tutelles></hal:affiliation><country>France</country></affiliation></author><author><name sortKey="Vera, Pierre" sort="Vera, Pierre" uniqKey="Vera P" first="Pierre" last="Vera">Pierre Vera</name><affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-23832" status="VALID"><orgName>Laboratoire d'Informatique, de Traitement de l'Information et des Systèmes</orgName><orgName type="acronym">LITIS</orgName><desc><address><addrLine>Avenue de l'Université UFR des Sciences et Techniques 76800 Saint-Etienne du Rouvray</addrLine><country key="FR"></country></address><ref type="url">http://www.litislab.eu</ref></desc><listRelation><relation active="#struct-300317" type="direct"></relation><relation name="EA4108" active="#struct-300318" type="direct"></relation><relation active="#struct-301288" type="direct"></relation><relation active="#struct-301232" type="indirect"></relation></listRelation><tutelles><tutelle active="#struct-300317" type="direct"><org type="institution" xml:id="struct-300317" status="VALID"><orgName>Université du Havre</orgName><desc><address><country key="FR"></country></address></desc></org></tutelle><tutelle name="EA4108" active="#struct-300318" type="direct"><org type="institution" xml:id="struct-300318" status="VALID"><orgName>Université de Rouen</orgName><desc><address><addrLine> 1 rue Thomas Becket - 76821 Mont-Saint-Aignan</addrLine><country key="FR"></country></address><ref type="url">http://www.univ-rouen.fr/</ref></desc></org></tutelle><tutelle active="#struct-301288" type="direct"><org type="department" xml:id="struct-301288" status="VALID"><orgName>Institut National des Sciences Appliquées - Rouen</orgName><orgName type="acronym">INSA Rouen</orgName><desc><address><country key="FR"></country></address></desc><listRelation><relation active="#struct-301232" type="direct"></relation></listRelation></org></tutelle><tutelle active="#struct-301232" type="indirect"><org type="institution" xml:id="struct-301232" status="VALID"><orgName>Institut National des Sciences Appliquées</orgName><orgName type="acronym">INSA</orgName><desc><address><country key="FR"></country></address></desc></org></tutelle></tutelles></hal:affiliation><country>France</country><placeName><settlement type="city">Le Havre</settlement><region type="region" nuts="2">Région Normandie</region><region type="old region" nuts="2">Haute-Normandie</region></placeName><orgName type="university">Université du Havre</orgName><placeName><settlement type="city">Rouen</settlement><region type="region" nuts="2">Région Normandie</region><region type="old region" nuts="2">Haute-Normandie</region></placeName><orgName type="university">Université de Rouen</orgName></affiliation></author><author><name sortKey="Bohn, Pierre" sort="Bohn, Pierre" uniqKey="Bohn P" first="Pierre" last="Bohn">Pierre Bohn</name><affiliation wicri:level="1"><hal:affiliation type="laboratory" xml:id="struct-23832" status="VALID"><orgName>Laboratoire d'Informatique, de Traitement de l'Information et des Systèmes</orgName><orgName type="acronym">LITIS</orgName><desc><address><addrLine>Avenue de l'Université UFR des Sciences et Techniques 76800 Saint-Etienne du Rouvray</addrLine><country key="FR"></country></address><ref type="url">http://www.litislab.eu</ref></desc><listRelation><relation active="#struct-300317" type="direct"></relation><relation name="EA4108" active="#struct-300318" type="direct"></relation><relation active="#struct-301288" type="direct"></relation><relation active="#struct-301232" type="indirect"></relation></listRelation><tutelles><tutelle active="#struct-300317" type="direct"><org type="institution" xml:id="struct-300317" status="VALID"><orgName>Université du Havre</orgName><desc><address><country key="FR"></country></address></desc></org></tutelle><tutelle name="EA4108" active="#struct-300318" type="direct"><org type="institution" xml:id="struct-300318" status="VALID"><orgName>Université de Rouen</orgName><desc><address><addrLine> 1 rue Thomas Becket - 76821 Mont-Saint-Aignan</addrLine><country key="FR"></country></address><ref type="url">http://www.univ-rouen.fr/</ref></desc></org></tutelle><tutelle active="#struct-301288" type="direct"><org type="department" xml:id="struct-301288" status="VALID"><orgName>Institut National des Sciences Appliquées - Rouen</orgName><orgName type="acronym">INSA Rouen</orgName><desc><address><country key="FR"></country></address></desc><listRelation><relation active="#struct-301232" type="direct"></relation></listRelation></org></tutelle><tutelle active="#struct-301232" type="indirect"><org type="institution" xml:id="struct-301232" status="VALID"><orgName>Institut National des Sciences Appliquées</orgName><orgName type="acronym">INSA</orgName><desc><address><country key="FR"></country></address></desc></org></tutelle></tutelles></hal:affiliation><country>France</country><placeName><settlement type="city">Le Havre</settlement><region type="region" nuts="2">Région Normandie</region><region type="old region" nuts="2">Haute-Normandie</region></placeName><orgName type="university">Université du Havre</orgName><placeName><settlement type="city">Rouen</settlement><region type="region" nuts="2">Région Normandie</region><region type="old region" nuts="2">Haute-Normandie</region></placeName><orgName type="university">Université de Rouen</orgName></affiliation></author></analytic><idno type="DOI">10.1016/j.bmcl.2013.05.015</idno></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="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.</div></front></TEI><affiliations><list><country><li>France</li></country><region><li>Haute-Normandie</li><li>Région Normandie</li></region><settlement><li>Le Havre</li><li>Rouen</li></settlement><orgName><li>Université de Rouen</li><li>Université du Havre</li></orgName></list><tree><noCountry><name sortKey="Castel, Helene" sort="Castel, Helene" uniqKey="Castel H" first="Hélène" last="Castel">Hélène Castel</name><name sortKey="Diouf, Cherif Bounana" sort="Diouf, Cherif Bounana" uniqKey="Diouf C" first="Chérif Bounana" last="Diouf">Chérif Bounana Diouf</name><name sortKey="Joyard, Yoann" sort="Joyard, Yoann" uniqKey="Joyard Y" first="Yoann" last="Joyard">Yoann Joyard</name></noCountry><country name="France"><region name="Région Normandie"><name sortKey="Le Joncour, Vadim" sort="Le Joncour, Vadim" uniqKey="Le Joncour V" first="Vadim" last="Le Joncour">Vadim Le Joncour</name></region><name sortKey="Bischoff, Laurent" sort="Bischoff, Laurent" uniqKey="Bischoff L" first="Laurent" last="Bischoff">Laurent Bischoff</name><name sortKey="Bohn, Pierre" sort="Bohn, Pierre" uniqKey="Bohn P" first="Pierre" last="Bohn">Pierre Bohn</name><name sortKey="Levacher, Vincent" sort="Levacher, Vincent" uniqKey="Levacher V" first="Vincent" last="Levacher">Vincent Levacher</name><name sortKey="Papamicael, Cyril" sort="Papamicael, Cyril" uniqKey="Papamicael C" first="Cyril" last="Papamicaël">Cyril Papamicaël</name><name sortKey="Vera, Pierre" sort="Vera, Pierre" uniqKey="Vera P" first="Pierre" last="Vera">Pierre Vera</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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