Complexes of Rhenium and Technetium with Chelating Thiourea Ligands PDF Download
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Languages : en
Pages : 200
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Author:
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Languages : en
Pages : 200
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Author: Hung Huy Nguyen
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Category :
Languages : en
Pages : 200
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Author: Jin-Hui Wang
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Category :
Languages : en
Pages : 281
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Rhenium complexes play a significant role in nuclear medicine. Rhenium has been widely used as a surrogate of technetium for a long time, and the promising physical features of 186Re and 188Re, make 186/188Re-complexes promising candidates as therapeutic radiopharmaceuticals.Similarly, the interesting photoactive and photoluminescence properties of non-radioactive Re-complexes make them excellent catalysts, luminescent materials and imaging sensors.Thus, in this work, our goal was to (i) develop, using a click chemistry strategy, multidentate ligands for the stabilization of different rhenium cores [Re(CO)3]+ and [ReO]3+ (M = Re or 188Re) as well as the analogous 99mTc-cores in some examples, (ii) assess the potential of the rhenium(technetium) complexes as imaging (natRe or 99mTc) or therapeutic (188Re) agents. To do so, two rhenium(technetium) specific-chelating systems were used: a semi-rigid tripodal system in the second chapter and a pyta moiety in the third chapter, these two chelators being developed previously in our group. Thus, based on a N2O tridentate click ligand, two different studies were carried out in chapter II. In the first one, two synthetic pathways to a range of potentially N3O tetradentate ligands, designed to coordinate rhenium cores as well as their coordination behaviors towards different rhenium cores (oxidation states +I and +V), were investigated. The first radiolabeling results combined with the recent work reported by Dugave and co-workers indicated that this ligand could be a promising 99mTc-chelator for nuclear imaging applications. As perspectives to this work, the extension of the radiolabelling work using the [188ReVO]3+ core should be performed, and the in vitro stability should be tested under physiological conditions in human plasma and by cysteine exchange experiments. The second study was focused on the development of novel hypoxia-selective 99mTc radiopharmaceuticals. Our semi-rigid tripodal click framework was decorated with an appended nitro group (either a nitrobenzyl group or a metronidazole (Mtz) unit). Different positions were considered and at least only two metronidazole (Mtz)-containing ligands and one nitro group-containing ligand as well as their corresponding tricarbonyl rhenium(I) complexes were obtained and characterized, in particular by electrochemistry. The reduction potentials of NO2 group in complexes [Re(CO)3Cl(L2)] and [Re(CO)3(L6)] were similar to those of reported hypoxic imaging agents, prompting us to further investigate other properties of these complexes. Chapter III was focused on the study of AIE (aggregation-induced emission) effect in tricarbonyl Re(I) complexes, the association of this effect with the intrinsic properties of Re(I) complexes being expected to lead to very attractive compounds. To do that, we combined an organic fluorophore (PBO) which exhibits excellent stability and optical properties, with a tricarbonylrhenium(I) complex based on a pyta unit (either a 2-pyridyl-1,2,3-triazole or a 2-pyridyl-1,2,4-triazole ligands). Four compounds were studied. The X-Ray structures revealed spectacular discrepancies between the two first triazole-based complexes ReL8 and ReL9. Moreover, this study being a novel orientation in our group, this work is a great starting point for further investigations. Various organic dyes and/or structural modifications of the organic moiety will soon be considered in order to develop highly emissive rhenium(I) luminescent probes.
Author: Christopher Alan Morse
Publisher:
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Category :
Languages : en
Pages : 334
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Author: John Anthony Thomas
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Category :
Languages : en
Pages : 262
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Author: Lauren L. Radford
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Category :
Languages : en
Pages : 119
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Technetium and rhenium have radioactive isotopes that are clinically useful for diagnostic (Tc-99m) or therapeutic (Re-186/188) purposes. This makes them attractive candidates for incorporation into pharmaceuticals. One way to incorporate radioactive metals into pharmaceuticals is through the use of a bifunctional chelating agent (BFCA), which inertly traps the metal while also attaching it to a targeting biomolecule. Technetium-99m is an attractive radionuclide not only because of its diagnostic capabilities, but also because it is a widely available and relatively affordable option. Two Tc-99m radiopharmaceuticals were created that seek to target somatostatin receptors (SSTRs), which are commonly overexpressed on neuroendocrine tumor tissues. Two different histidine-derived BFCAs were used to chelate a technetium-99m tricarbonyl core while simultaneously tethering it to an antagonist peptide with a high affinity for somatostatin receptor subtype two (SSTR2). Due to the fact that non-radioactive Re is in the same group as Tc, the analogous macroscale Re compounds were synthesized. This helped to determine the identity of the products made on the radiotracer level (nano- to picomolar) as well as determine receptor affinity through competitive binding assays in SSTR2-expressing cells. Both Re compounds, exhibited very good, low nanomolar affinities for SSTR2. The Tc-99m radiotracer products both exhibited high in vitro stability during challenges in cysteine, histidine, and mouse serum. Biodistribution and imaging studies in mice were also performed. The complexation of Re using a tetradentate diphosphinedithiol (DPDT) ligand was also explored. Rhenium is more readily oxidized than technetium, which can cause complications when seeking to use Re-186/188 radiopharmaceuticals in the body. Complexation with more reducing ligands (such as DPDT) may help stabilize Re(V) in the body. Thus, the initial chemistry of Re- and Tc-DPDT complexes was explored. This led to the creation of a highly stable Re(V)-DPDT complex, which remained stable in oxidative environments over a period of several months. Macroscale reactions using the DPDT ligand to synthesize the Tc-99 counterpart led to the formation of Tc(III) complexes from Tc(VII), without the need for additional reducing agents.
Author: Maciej Chotkowski
Publisher: Springer Nature
ISBN: 3030628639
Category : Science
Languages : en
Pages : 162
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This book provides detailed information on the electrochemistry of technetium compounds. After a brief physico-chemical characterization of this element, it presents the comparative chemistry of technetium, manganese and rhenium. Particular attention is paid to the stability, disproportionation, comproportionation, hydrolysis and polymerization reactions of technetium ions and their influence on the observed redox systems. The electrochemical properties of both inorganic as well as organic technetium species in aqueous and non-aqueous solutions are also discussed. The respective chapters cover the whole spectrum of topics related to the application of technetium in nuclear medicine, electrochemistry of technetium in spent nuclear fuel (including corrosion properties of technetium alloys), and detecting trace amounts of technetium with the aid of electrochemical methods. Providing readers with information not easily obtained in any other single source, the book will appeal to researchers working in nuclear chemistry, nuclear medicine or the nuclear industry.
Author: Raymond Dixon Peacock
Publisher:
ISBN:
Category : Rhenium
Languages : en
Pages : 156
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Author: Ali Barandov
Publisher:
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Category :
Languages : en
Pages : 287
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Author: Kenji Yoshihara
Publisher: Springer
ISBN: 9783662148488
Category : Science
Languages : en
Pages : 301
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