Rhenium and Technetium Complexes with Tridentate S,N, O Ligands Derived from Benzoylhydrazine PDF Download
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Author:
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Category : Rhenium
Languages : en
Pages : 8
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Author:
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Category : Rhenium
Languages : en
Pages : 8
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Author: John Anthony Thomas
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Category :
Languages : en
Pages : 262
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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: Raymond Dixon Peacock
Publisher:
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Category : Rhenium
Languages : en
Pages : 156
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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.
![The Coordination Chemistry of Technetium and Rhenium and Applications to Nuclear Medicines. [Annual] Technical Report, April 1, 1993--December 31, 1993 PDF](https://books.google.com/books/content/images/frontcover/kY-UDAEACAAJ?fife=w80-h100)
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Languages : en
Pages : 9
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The dramatic dependence of Re-binding to functionalized hydrazines on the nature of the coligands associated with the metal site has led to an examination of alkoxy and thiolato ligand types. The observation that multidentate thiolate ligands are highly effective in this latter role suggests the design and synthesis of new chelating polythiolate ligands with high binding affinities for radiometallic nuclides and of functionalized polythiolate ligands for the preparation of radionuclide-conjugated antibodies or peptides and the preparation and characterization of their complexes not only with the Group 7 metals Tc and Re but with the Group 13 metals Ga and In, which also possess radionuclides with useful properties. Since the rational design of these novel bifunctional conjugates requires a fundamental understanding of the coordination chemistry of relevant metals with polythiolate ligands whose syntheses and properties remain unexplored, effort has been directed toward the preparation of novel polythiolate ligands and the characterization of their complexes with Group 7 and Group 13 metals. This report describes studies on several complementary aspects of the coordination chemistry of the pyridinethiolate derived ligands 2-HSC5NH3-SiR3, 2-HSC5NH3-6-SiR3 and 2-HSC5NH2-3,6-SiR3 and the potentially bifunctional polythiolate ligand HOOCCH2Si(CH2CH2SH)3 have been synthesized; of several aspects of rhenium-hydrazido and rhenium-thiolate chemistry have been developed; of Ga and In complexes of the 2-pyridinethiolate class of ligands have been synthesized and structurally characterized; and of the general coordination properties of the 2-pyrithinethiolate and related ligand types.
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Category :
Languages : en
Pages : 200
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Author: Ali Barandov
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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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Author: Christopher Alan Morse
Publisher:
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Category :
Languages : en
Pages : 334
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