In vivo and in vitro studies of [M(η6-pseudoerlotinib)2]+ sandwich complexes (M = Re, 99mTc)

Battistin, Federica; Fernandes, Célia; Raposinho, Paula. D.; Blacque, Olivier; Paulo, António; Alberto, Roger

doi:10.1039/d3dt03011c

Dalton Trans.

2023

DOI: 10.1039/d3dt03011c

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In vivo and in vitro studies of [M(η⁶-pseudoerlotinib)₂]⁺ sandwich complexes (M = Re, ^99mTc)

Federica Battistin,

Célia Fernandes,

Paula. D. Raposinho

et al.

Abstract: The pursuit of molecular imaging for tumors has led to endeavors focused on targeting epidermal growth factor receptors (EGFR) through monoclonal antibodies or radioisotope-labelled EGF analogs with 99mTc, 111In, or...

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2024

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Synthesis, Characterization, and Biological Evaluation of Novel [M(η⁶-arene)₂]⁺ (M = Re, ^99mTc) Hosted Terpyridines and Copper Complexes Thereof

Csucker,

Scarpi-Luttenauer,

Mesdom

et al. 2024

Inorg. Chem.

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We report the synthesis, characterization, and in vitro biological activities of [Re(η 6 -arene) 2 ] + -terpyridine conjugates and their Cu II complexes. The terpyridine (terpy) chelators were attached to the [Re(η 6 -arene) 2 ] + scaffold via secondary amine linkers allowing for heteroleptic mono-and homoleptic bisterpyridine-substituted chelators. Complexation with CuCl 2 afforded the respective square pyramidal [Cu(terpy)Cl 2 ] complexes hosted on the [Re(η 6 -arene) 2 ] + scaffold. The chelator conjugates and their respective complexes were found to be remarkably cytotoxic against malignant HT29 and A549 human cancer cell lines in vitro with IC 50 values in the low micromolar range. Mitochondrial respiration disruption was identified as a possible mode of action of these novel drug candidates. Crucially, the [Re(η 6 -arene) 2 ] + hosts delivered water solubility of the otherwise insoluble [Cu(terpy)Cl 2 ] motif. Importantly, the homoleptic [ 99m Tc(η 6 -arene) 2 ] + -terpyridine conjugate is available in a single step, which enables the presented system to be used as a theranostic approach to modern medicinal inorganic chemistry.

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Synthesis, Characterization, and Biological Evaluation of Novel [M(η⁶-arene)₂]⁺ (M = Re, ^99mTc) Hosted Terpyridines and Copper Complexes Thereof

Csucker,

Scarpi-Luttenauer,

Mesdom

et al. 2024

Inorg. Chem.

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In vivo and in vitro studies of [M(η⁶-pseudoerlotinib)₂]⁺ sandwich complexes (M = Re, ^99mTc)

Abstract: The pursuit of molecular imaging for tumors has led to endeavors focused on targeting epidermal growth factor receptors (EGFR) through monoclonal antibodies or radioisotope-labelled EGF analogs with 99mTc, 111In, or...

Cited by 1 publication

References 27 publications

Synthesis, Characterization, and Biological Evaluation of Novel [M(η⁶-arene)₂]⁺ (M = Re, ^99mTc) Hosted Terpyridines and Copper Complexes Thereof

Synthesis, Characterization, and Biological Evaluation of Novel [M(η⁶-arene)₂]⁺ (M = Re, ^99mTc) Hosted Terpyridines and Copper Complexes Thereof

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In vivo and in vitro studies of [M(η6-pseudoerlotinib)2]+ sandwich complexes (M = Re, 99mTc)

Abstract: The pursuit of molecular imaging for tumors has led to endeavors focused on targeting epidermal growth factor receptors (EGFR) through monoclonal antibodies or radioisotope-labelled EGF analogs with 99mTc, 111In, or...

Cited by 1 publication

References 27 publications

Synthesis, Characterization, and Biological Evaluation of Novel [M(η6-arene)2]+ (M = Re, 99mTc) Hosted Terpyridines and Copper Complexes Thereof

Synthesis, Characterization, and Biological Evaluation of Novel [M(η6-arene)2]+ (M = Re, 99mTc) Hosted Terpyridines and Copper Complexes Thereof

Contact Info

Product

Resources

About

In vivo and in vitro studies of [M(η⁶-pseudoerlotinib)₂]⁺ sandwich complexes (M = Re, ^99mTc)

Synthesis, Characterization, and Biological Evaluation of Novel [M(η⁶-arene)₂]⁺ (M = Re, ^99mTc) Hosted Terpyridines and Copper Complexes Thereof

Synthesis, Characterization, and Biological Evaluation of Novel [M(η⁶-arene)₂]⁺ (M = Re, ^99mTc) Hosted Terpyridines and Copper Complexes Thereof