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Fluorescent gallium and indium bis(thiosemicarbazonates) and their radiolabelled analogues : synthesis, structures and cellular confocal fluorescence imaging investigations

Arrowsmith, Rory L. and Waghorn, Philip A. and Jones, Michael W. and Bauman, Andreas and Brayshaw, Simon K. and Hu, Zhiyuan and Kociok-Köhn, Gabriele and Mindt, Thomas L. and Tyrrell, Rex M. and Botchway, Stanley W. and Dilworth, Jonathan R. and Pascu, Sofia I.. (2011) Fluorescent gallium and indium bis(thiosemicarbazonates) and their radiolabelled analogues : synthesis, structures and cellular confocal fluorescence imaging investigations. Dalton transactions, Vol. 40, H. 23. pp. 6238-6252.

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Official URL: http://edoc.unibas.ch/dok/A6004756

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Abstract

New fluorescent and biocompatible aromatic Ga(III)- and In(III)-bis(thiosemicarbazonato) complexes for dual mode optical and PET or SPECT molecular imaging have been synthesised via a synthetic method based on transmetallation reactions from Zn(II) precursors. Complexes have been fully characterised in the solid state by single crystal X-ray diffraction and in solution by spectroscopic methods (UV/Vis, fluorescence, (1)H and (13)C{(1)H} NMR). The bis(thiosemicarbazones) radiolabelled rapidly in high yields under mild conditions with (111)In (a gamma and Auger emitter for SPECT imaging and radiotherapy with t(1/2) = 2.8 d) and (68)Ga (a generator-available positron emitter for PET imaging with t(1/2) = 68 min). Cytotoxicity and biolocalisation studies using confocal fluorescence imaging and fluorescence lifetime imaging (FLIM) techniques have been used to study their in vitro activities and stabilities in HeLa and PC-3 cells to ascertain their suitability as synthetic scaffolds for future multimodality molecular imaging in cancer diagnosis and therapy. The observation that the indium complexes show certain nuclear uptake could be of relevance towards developing (111)In therapeutic agents based on Auger electron emission to induce DNA damage.
Faculties and Departments:03 Faculty of Medicine > Bereich Querschnittsfächer (Klinik) > Ehemalige Einheiten Querschnittsfächer (Klinik) > Radiologische Chemie (Mindt)
03 Faculty of Medicine > Departement Klinische Forschung > Bereich Querschnittsfächer (Klinik) > Ehemalige Einheiten Querschnittsfächer (Klinik) > Radiologische Chemie (Mindt)
UniBasel Contributors:Mindt, Thomas L.
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Royal Society of Chemistry
ISSN:1477-9226
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:27 Feb 2014 15:45
Deposited On:27 Feb 2014 15:45

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