Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Rebekka Hueting; Martin Christlieb; Jonathan R. Dilworth; Elisa García Garayoa; Véronique Gouverneur; Michael W. Jones; Veronique Maes; Roger Schibli; Xin Sun; Dirk A. Tourwé

doi:10.1039/B925128F

Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copperlabeling of peptides†

Rebekka Hueting,^ac Martin Christlieb,*^c Jonathan R. Dilworth,*^a Elisa García Garayoa,^b Véronique Gouverneur,^a Michael W. Jones,^a Veronique Maes,^d Roger Schibli,^b Xin Sun^a and Dirk A. Tourwé^d

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^a Department of Chemistry, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford, United Kingdom
E-mail: jon.dilworth@chem.ox.ac.uk
Fax: +44 (0)1865 272690
Tel: +44 (0)1865 272689

^b Paul Scherrer Institute, Centre for Radiopharmaceutical Science, Villigen, Switzerland

^c Gray Institute for Radiation Oncology and Biology, University of Oxford, Old Road Campus Research Bldg., Old Road Campus, Oxford, United Kingdom
E-mail: martin.christlieb@rob.ox.ac.uk

^d Department of Organic Chemistry, Vrije Universiteit Brussels, Brussels, Belgium

Abstract

A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both ⁶⁴Cu and ^99mTc. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic methodologies and the ⁶⁴Cu-labeled conjugate was shown to have good tumour uptake in mice with xenografted PC-3 tumours.

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Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copperlabeling of peptides†

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