Issue 23, 2022

To chelate thallium(i) – synthesis and evaluation of Kryptofix-based chelators for 201Tl

Abstract

While best known for its toxic properties, thallium has also been explored for applications in nuclear diagnostics and medicine. Indeed, [201Tl]TlCl has been used extensively for nuclear imaging in the past before it was superceded by other radionuclides such as 99mTc. One reason for this loss of interest is the severe lack of suitable organic chelators able to effectively coordinate ionic forms of Tl and deliver it to specific diseased tissue by means of attached biological vectors. Herein, we describe the synthesis and characterisation of a series of Kryptofix 222-based chelators that can be radiolabelled with 201Tl(I) in high radiochemical yields at ambient temperature. We demonstrate that from these simple chelators, targeted derivatives are readily accessible and describe the synthesis and preliminary biological evaluation of a PSMA-targeted 201Tl-labelled Kryptofix 222-peptide conjugate. While the Kryptofix system is demonstrably capable of binding the thallium cation, no PSMA-mediated cell-uptake could be detected with the PSMA conjugate, suggesting that this targeting moiety may not be ideal for use in conjunction with 201Tl.

Graphical abstract: To chelate thallium(i) – synthesis and evaluation of Kryptofix-based chelators for 201Tl

Supplementary files

Article information

Article type
Paper
Submitted
07 апр 2022
Accepted
21 май 2022
First published
23 май 2022
This article is Open Access
Creative Commons BY license

Dalton Trans., 2022,51, 9039-9048

To chelate thallium(I) – synthesis and evaluation of Kryptofix-based chelators for 201Tl

A. Frei, A. Rigby, T. T. C. Yue, G. Firth, M. T. Ma and N. J. Long, Dalton Trans., 2022, 51, 9039 DOI: 10.1039/D2DT01074G

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