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Rhenium and Technetium-oxo Complexes with Thioamide Derivatives of Pyridylhydrazine Bifunctional Chelators Conjugated to the Tumour Targeting Peptides Octreotate and Cyclic-RGDfK

Research output: Contribution to journalArticle

Andrea J North, John A Karas, Michelle T Ma, Philip J Blower, Uwe Ackermann, Jonathan M White, Paul S Donnelly

Original languageEnglish
Pages (from-to)9725-9741
Number of pages17
JournalINORGANIC CHEMISTRY
Volume56
Issue number16
DOIs
Published21 Aug 2017

Documents

  • acs.inorgchem.7b01247

    acs.inorgchem.7b01247.pdf, 2.02 MB, application/pdf

    Uploaded date:11 Sep 2017

    Version:Final published version

    Licence:CC BY

King's Authors

Abstract

This research aimed to develop new tumor targeted theranostic agents taking advantage of the similarities in coordination chemistry between technetium and rhenium. A γ-emitting radioactive isotope of technetium is commonly used in diagnostic imaging, and there are two β(-) emitting radioactive isotopes of rhenium that have the potential to be of use in radiotherapy. Variants of the 6-hydrazinonicotinamide (HYNIC) bifunctional ligands have been prepared by appending thioamide functional groups to 6-hydrazinonicotinamide to form pyridylthiosemicarbazide ligands (SHYNIC). The new bidentate ligands were conjugated to the tumor targeting peptides Tyr(3)-octreotate and cyclic-RGD. The new ligands and conjugates were used to prepare well-defined {M═O}(3+) complexes (where M = (99m)Tc or (nat)Re or (188)Re) that feature two targeting peptides attached to the single metal ion. These new SHYNIC ligands are capable of forming well-defined rhenium and technetium complexes and offer the possibility of using the (99m)Tc imaging and (188/186)Re therapeutic matched pairs.

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