Novel Rhenium and Technetium Metal Complexes of N-centred Tripodal Phosphine Ligands Towards SPECT Imaging PDF Download
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Author: Saul Cooper
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Languages : en
Pages :
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Author: Saul Cooper
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Languages : en
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Author: Ali Barandov
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Category :
Languages : en
Pages : 287
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Author: Jin-Hui Wang
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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: John Anthony Thomas
Publisher:
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Category :
Languages : en
Pages : 262
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Author: Mattia Riondato
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Languages : en
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Author: Benjamin B. Kasten
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Languages : en
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The third study developed isothiocyanate-functionalized DPA ligands and fac-[MI(CO)3]+ complexes for conjugation reactions with amine-containing biomolecules. Utilizing lysine as a preliminary model for peptide-based biomolecules established the proof of concept that the isothiocyanate derivatives could be used to prepare targeted radiopharmaceuticals. Finally, strategies utilizing phosphine ligands with fac-[MI(CO)3]+ complexes were developed and showed potential for use with targeting agents in future endeavors.
Author: Steven J. Mather
Publisher: Springer Science & Business Media
ISBN: 9400917686
Category : Medical
Languages : en
Pages : 248
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Radiophannaceutical research has recently undergone a major change in direction. In past years it has been concerned mainly with the development of perfusion tracers, the biodistribution of which reflect the regional blood flow to areas of major organs such as the heart and brain. However, a major new direction of interest now lies in the development of receptor-binding radio-tracers which can be used to perform in-vivo characterisation of diseased tissues and it is likely that much of the future research in this field will follow this direction. The difficulties in developing such tracers are considerable. The researcher must first identify a promising target for radiopharmaceutical development. High specific activity radioactive molecules must be designed and synthesised which will both bind to the target receptor with high affinity, and also have the physicochemical characteristics which will allow them to reach the target site in sufficient quantity while at the same time showing minimal uptake in non-target tissues. Thus the knowledge base required for radiophannaceutical development has now expanded beyond the limits of radiopharmaceutical chemistry to include aspects of biochemistry, molecular biology and conventional drug design. The portfolio of basic knowledge required to support current radiopharmaceutical development is changing and scientists working in this arena need to be trained in this regard. At the same time, the very latest developments in the field need to be communicated to the scientific community in order to stimulate the advancement of this exciting new direction of research.
Author: Surinder K. Mehta
Publisher: John Wiley & Sons
ISBN: 3527348689
Category : Science
Languages : en
Pages : 292
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Metallosurfactants Provides up-to-date coverage of the synthesis, properties, and applications of metallosurfactants Metallosurfactants: From Fundamentals to Catalytic and Biomedical Applications is a thorough introduction to amphiphilic compounds that allow to incorporate metal ions in the surfactant system. This comprehensive reference and guide describes the fundamentals of metal surfactant complexes, highlights recent advances in the field, and explores current and future applications and research areas. Gradually progressing from basic to advanced topics, the authors first explain the classification and characterization of metallosurfactants before delving into more complex concepts and various catalytic, sensing, and biomedical applications. The book begins with coverage of the synthesis of metallosurfactants and their surface, interfacial, and aggregation behavior. Subsequent chapters discuss applications of metallosurfactants in areas such as drug delivery, molecular machines, transfection, nanoparticle synthesis, and carbon monoxide-releasing molecules (CORMs). Other topics include the use of metallosurfactants as catalysts in organic reactions, and as anticancer and antimicrobial agents in drug delivery and formulation. This unique reference Provides an overview of the structure-function relationship, synthesis methods, and characterization of metallosurfactants Reviews current trends in metallosurfactant development and research Examines the use of metallosurfactants in a wide range of reactions, including esterolytic reactions and hydrogen generation Discusses advanced applications of metallosurfactants, e.g. as nanoreactors for nanoparticle synthesis, non-viral transfection vectors, and sensors Metallosurfactants: From Fundamentals to Catalytic and Biomedical Applications is an excellent introduction to the growing field of metallosurfactant chemistry as well as a concise, highly useful reference for researchers and scientists in both academia and industry.
Author: IAEA.
Publisher:
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Category :
Languages : en
Pages : 378
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Technetium-99m radiopharmaceuticals will continue to have a significant impact in several areas of nuclear medicine. This publication is intended to provide a broad overview of the current status of technetium-99m radiopharmaceuticals. It includes chapters on the most advanced chemical techniques for labelling biomolecules and synthesizing suitable multifunctional ligands that will help in the development of specific radiotracers. Of special interest for the reader are details of recent research to develop technetium-99m tracers for monitoring different biological processes enabling the develo.
Author: Ilse Zolle
Publisher: Springer Science & Business Media
ISBN: 3540339906
Category : Medical
Languages : en
Pages : 354
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Radioactive drug development is a multi-disciplinary task. Therefore, dedicated scientists and experts from different fields of specialisation have contributed to this book. The text reviews forty years of advances in radiopharmaceutical development based on Technetium. The first section reviews basic principles and analytic methods, and information on chemical makeup of radiopharmaceuticals. Part 2 reviews 99mTc-radiopharmaceuticals used in nuclear medicine, thoroughly outlining their chemistry, formulation, pharmacokinetics and clinical applications.
