Issue 23, 2011

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

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, 1H and 13C{1H} NMR). The bis(thiosemicarbazones) radiolabelled rapidly in high yields under mild conditions with 111In (a gamma and Auger emitter for SPECT imaging and radiotherapy with t1/2 = 2.8 d) and 68Ga (a generator-available positron emitter for PET imaging with t1/2 = 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 111In therapeutic agents based on Auger electron emission to induce DNA damage.

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

Supplementary files

Article information

Article type
Paper
Submitted
21 Jan 2011
Accepted
05 May 2011
First published
19 May 2011

Dalton Trans., 2011,40, 6238-6252

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

R. L. Arrowsmith, P. A. Waghorn, M. W. Jones, A. Bauman, S. K. Brayshaw, Z. Hu, G. Kociok-Köhn, T. L. Mindt, R. M. Tyrrell, S. W. Botchway, J. R. Dilworth and S. I. Pascu, Dalton Trans., 2011, 40, 6238 DOI: 10.1039/C1DT10126A

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