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Issue 42, 2017
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Thiourea derivatives as chelating agents for bioconjugation of rhenium and technetium

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Abstract

Potential tetradentate thiocarbamoylbenzamidine derivatives H4L have been synthesized from the corresponding benzimidoyl chlorides and triglycine. They are suitable chelating agents for the oxidotechnetium(V) and oxidorhenium(V) cores and form stable, neutral [MO(HL)] complexes with an equatorial SN3 coordination sphere and an additional, uncoordinated carboxylic group, which can be used for bioconjugation. Representatives of the rhenium and 99Tc products have been isolated and analyzed with spectroscopic methods and X-ray diffraction. Bioconjugates of these complexes with angiotensin-II have been synthesized and structurally characterized. Analogous 99mTc complexes have been produced and tested in vitro and in vivo. The experiments confirm a considerable stability for the [99mTc(HL)] product as well as for its bioconjugate and recommend this class of compounds for further bioconjugation studies towards clinical applications.

Graphical abstract: Thiourea derivatives as chelating agents for bioconjugation of rhenium and technetium

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Supplementary files

Article information


Submitted
19 May 2017
Accepted
15 Jun 2017
First published
22 Jun 2017

Dalton Trans., 2017,46, 14602-14611
Article type
Paper

Thiourea derivatives as chelating agents for bioconjugation of rhenium and technetium

J. D. C. Gomez, A. Hagenbach, U. I. M. Gerling-Driessen, B. Koksch, N. Beindorff, W. Brenner and U. Abram, Dalton Trans., 2017, 46, 14602
DOI: 10.1039/C7DT01834G

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