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Title: Rhenium and technetium-oxo complexes with thioamide derivatives of pyridylhydrazine bifunctional chelators conjugated to the tumour targeting peptides octreotate and cyclic-RGDfK
Authors: North, Andrea J;Karas, John A;Ma, Michelle T;Blower, Philip J;Ackermann, Uwe;White, Jonathan M;Donnelly, Paul S
Issue Date: 21-Aug-2017
EDate: 2017-08-02
Citation: Inorganic Chemistry 2017; 56(16): 9725-9741
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 Tyr3-octreotate and cyclic-RGD. The new ligands and conjugates were used to prepare well-defined {M═O}3+ complexes (where M = 99mTc or natRe or 188Re) 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 99mTc imaging and 188/186Re therapeutic matched pairs.
DOI: 10.1021/acs.inorgchem.7b01247
ORCID: 0000-0002-0707-6257
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Type: Journal Article
Appears in Collections:Journal articles

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