Modification of Biodistribution and Brain Uptake of Copper Bis(thiosemicarbazonato) Complexes by the Incorporation of Amine and Polyamine Functional Groups

Brett M Paterson; Carleen Cullinane; Peter J Crouch; Anthony R White; Kevin J Barnham; Peter D Roselt; Wayne Noonan; David Binns; Rodney J Hicks; Paul S Donnelly

Journal article

Modification of Biodistribution and Brain Uptake of Copper Bis(thiosemicarbazonato) Complexes by the Incorporation of Amine and Polyamine Functional Groups

Brett M Paterson, Carleen Cullinane, Peter J Crouch, Anthony R White, Kevin J Barnham, Peter D Roselt, Wayne Noonan, David Binns, Rodney J Hicks, Paul S Donnelly

INORGANIC CHEMISTRY | AMER CHEMICAL SOC | Published : 2019

DOI: 10.1021/acs.inorgchem.9b00117

Abstract

The synthesis of new bis(thiosemicarbazonato)copper(II) complexes featuring polyamine substituents via selective transamination reactions is presented. Polyamines of different lengths, with different ionizable substituent groups, were used to modify and adjust the hydrophilic/lipophilic balance of the copper complexes. The new analogues were radiolabeled with copper-64 and their lipophilicities estimated using distribution coefficients. The cell uptake of the new polyamine complexes was investigated with preliminary in vitro biological studies using a neuroblastoma cancer cell line. The in vivo biodistribution of three of the new analogues was investigated in vivo in mice using positron-emis..

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University of Melbourne Researchers

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Grants

Funding Acknowledgements

We thank the Australian Research Council for funding aspects of this research. We thank Irene Volitakis for her expertise in ICP-MS analysis of the cells. We thank Kerry Ardley and Susan Jackson for their technical expertise in performing the PET scanning. We thank Charmaine M. Jeffery and Roger I. Price (Department of Medical Technology and Physics, Sir Charles Gairdner Hospital, Nedlands, Western Australia, Australia) for the provision of copper-64.