Synthesis and reactions of trigonal-bipyramidal rhenium and technetium complexes with a tripodal, tetradentate NS3 ligand

Spies, Hartmut; Glaser, Matthias; Pietzsch, Hans‐Jürgen; Hahn, F. Ekkehardt; Lügger, Thomas

doi:10.1016/0020-1693(95)04571-6

Cited by 69 publications

(51 citation statements)

References 33 publications

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“…The tetradentate NS 3 ligand (2,2’,2’’-nitrilotriethanethiol) was prepared by reaction of tris(2-chloroethyl)amine hydrochloride with potassium thioacetate followed by reduction with LiAlH 4 [ 24 ]. The substrates for the synthesis of NS 3 ligand were benzyl bromide (Merck, Darmstadt, Germany), ethylene sulphide (Merck, Darmstadt, Germany) and S-benzyl-L-cysteine (Fluka, Mexico City, Mexico) compounds.…”

Section: Methodsmentioning

confidence: 99%

Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

et al. 2018

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Gliomas, particularly WHO grade IV glioblastoma multiforme, are one of the most common and aggressive primary tumors of the central nervous system. The neuropeptide, substance P (SP), is the physiological ligand of the neurokinin-1 (NK-1) receptor that is consistently overexpressed in glioblastoma cells. The aim of this work was to study physico-chemical and biological properties of different SP analogues labeled with technetium-99m and lutetium-177 radionuclides. The synthesized compounds were characterized in vitro by partition coefficients (logP) and their stability was investigated in various physiological solutions. Biological properties (Kd, Bmax) were characterized using the U373 MG cell line. The obtained lipophilicity values of the [99mTc]NS3/CN-SP and [177Lu]DOTA-SP radiobioconjugates were in the range of −0.3 to +0.6 and −2.5 to −5.0, respectively. The studied radiobioconjugates were stable in PBS buffer and CSF, as well as in 10 mM histidine and/or cysteine solutions whereas in human serum showed enzymatic biodegradation. [177Lu]DOTA-[Thi8,Met(O2)11]SP(1–11), [177Lu]DOTA-SP(4–11) and [177Lu]DOTA-[Thi8,Met(O2)11]SP(5–11) radiobioconjugates bound specifically to NK-1 receptors expressed on glioblastoma cells with affinity in the nanomolar range. To conclude, the shorter analogues of SP can be used as vectors, nevertheless they still do not fulfil all requirements for preparations in nuclear medicine.

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Section: Methodsmentioning

confidence: 99%

Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

et al. 2018

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“…The synthesis of the hexathiourea Re(III) precursor complex [Re(tu) 6 ]Cl 3 Â 4H 2 O (tu ¼ SC(NH 2 ) 2 ) was carried out according to Gambino et al [26]. The Re(III)-dimethyl phenyl phosphino complex [Re(NS 3 )(PMe 2 Ph)] was prepared as published by Spies et al [27].…”

Section: Methodsmentioning

confidence: 99%

Novel 99mTc ‘4 + 1’ peptide conjugates: Tuning the biodistribution by variation of coligands

Kunstler¹,

Seidel

Bergmann

et al. 2010

European Journal of Medicinal Chemistry

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“…The title compound was prepared according to the method published by Spies et al (1995). Slow solvent evaporation of a solution of (I) in chloroform-acetone-cyclohexane (8:1:1) gave green crystals suitable for X-ray analysis.…”

Section: Methodsmentioning

confidence: 99%

[2-Carboxy-2,2′,2′′-nitrilotris(ethanethiolato)-κ⁴N,S,S′,S′′](triphenylphosphine-κP)rhenium(III) acetone solvate

Schiller¹,

Kraus²,

Reck³

et al. 2005

Acta Cryst E

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Synthesis and reactions of trigonal-bipyramidal rhenium and technetium complexes with a tripodal, tetradentate NS3 ligand

Cited by 69 publications

References 33 publications

Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

Novel 99mTc ‘4 + 1’ peptide conjugates: Tuning the biodistribution by variation of coligands

[2-Carboxy-2,2′,2′′-nitrilotris(ethanethiolato)-κ⁴N,S,S′,S′′](triphenylphosphine-κP)rhenium(III) acetone solvate

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Synthesis and reactions of trigonal-bipyramidal rhenium and technetium complexes with a tripodal, tetradentate NS3 ligand

Cited by 69 publications

References 33 publications

Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

Application of Neurokinin-1 Receptor in Targeted Strategies for Glioma Treatment. Part I: Synthesis and Evaluation of Substance P Fragments Labeled with 99mTc and 177Lu as Potential Receptor Radiopharmaceuticals

Novel 99mTc ‘4 + 1’ peptide conjugates: Tuning the biodistribution by variation of coligands

[2-Carboxy-2,2′,2′′-nitrilotris(ethanethiolato)-κ4N,S,S′,S′′](triphenylphosphine-κP)rhenium(III) acetone solvate

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[2-Carboxy-2,2′,2′′-nitrilotris(ethanethiolato)-κ⁴N,S,S′,S′′](triphenylphosphine-κP)rhenium(III) acetone solvate