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 13C1H} 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.
新型荧光和
生物相容性芳香族Ga(III)和In(III)双(
氨基
硫代半卡巴脒)配合物已通过基于从Zn(II)前体进行的
金属转移反应的合成方法合成,适用于双模式光学和PET或
SPECT分子成像。配合物在固态下通过单晶X射线衍射和在溶液中通过光谱方法(UV/Vis、荧光、1H和13C1H} NMR)进行了全面表征。双(
氨基
硫代半卡巴脒)在温和条件下快速高效地进行111In(用于
SPECT成像和放射治疗的γ和俄歇发射体,t1/2 = 2.8 d)和68Ga(用于PET成像的发生器可用正电子发射体,t1/2 = 68 min)的放射性标记。采用共聚焦
荧光成像和荧光寿命成像(FLIM)技术进行的细胞毒性和
生物定位研究,用于研究它们在HeLa和PC-3细胞中的体外活性和稳定性,以确定它们作为未来癌症诊断和治疗中多模式分子成像合成骨架的适用性。观察到
铟配合物显示出一定的核摄取,这对于开发基于俄歇电子发射诱导DNA损伤的111In治疗剂可能具有相关性。