title: Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.
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.
authors.affiliation: Department of Nuclear Medicine, Henri Becquerel Center and Rouen University Hospital and QuantIF-LITIS (EA4108), 1 rue d'Amiens, 76038 Rouen Cedex, France.
authors.forename: Yoann
authors.initials: Y
authors.lastname: Joyard
authors.forename: Vadim
authors.initials: V
authors.lastname: Le Joncour
authors.forename: Hélène
authors.initials: H
authors.lastname: Castel
authors.forename: Chérif Bounana
authors.initials: CB
authors.lastname: Diouf
authors.forename: Laurent
authors.initials: L
authors.lastname: Bischoff
authors.forename: Cyril
authors.initials: C
authors.lastname: Papamicaël
authors.forename: Vincent
authors.initials: V
authors.lastname: Levacher
authors.forename: Pierre
authors.initials: P
authors.lastname: Vera
authors.forename: Pierre
authors.initials: P
authors.lastname: Bohn
mesh_terms: D000818:Animals; D015687:Cell Hypoxia; D045744:Cell Line, Tumor; D005909:Glioblastoma / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D014018:Tissue Distribution
chemical_list: C403973:BRU 59-21; D007093:Imidazoles; D015609:Organotechnetium Compounds