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Anti Cancer N Heterocyclic Carbene Complexes Of Goldiii Goldi And Platinumii
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Book Synopsis Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II) by : Taotao Zou
Download or read book Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II) written by Taotao Zou and published by Springer. This book was released on 2016-02-19 with total page 175 pages. Available in PDF, EPUB and Kindle. Book excerpt: This thesis focuses on the development of gold- and non-classical platinum-based anti-cancer agents that display distinctively different anti-cancer mechanisms compared to the commonly used cisplatin. These metal complexes contain N-heterocyclic carbene (NHC) ligands which are able to form strong M-C(NHC) bonds, conferring high stability and favorable lipophilicity, reactivity and binding specificity of metal complexes on biomolecules. The author demonstrates significant advances made in anti-cancer gold(III), gold(I) and platinum(II) complexes. Detailed chemical synthesis, in vitro and/or in vivo anti-cancer activities are clearly presented including: (i) a class of Au(III) complexes containing a highly fluorescent N^N^N ligand and NHC ligand that simultaneously act as fluorescent thiol “switch-on” probes and anti-cancer agents; (ii) a dinuclear gold(I) complex with a mixed diphosphine and bis(NHC) ligand displaying favorable stability and showing significant inhibition of tumor growth in two independent mice models with no observable side effects; and (iii) a panel of stable luminescent cyclometalated platinum(II) complexes exhibiting high specificity to localize to the endoplasmic reticulum (ER) domain, inducing ER stress and cell apoptosis. These works highlight the clinical potential that gold and platinum complexes offer for cancer treatment.
Book Synopsis Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(iii), Gold(i) and Platinum(ii) by : Taotao Zou
Download or read book Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(iii), Gold(i) and Platinum(ii) written by Taotao Zou and published by Open Dissertation Press. This book was released on 2017-01-27 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: This dissertation, "Anti-cancer N-heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II): Thiol "switch-on" Fluorescent Probes, Thioredoxin Reductase Inhibitors and Endoplasmic Reticulum Targeting Agents" by Taotao, Zou, 邹滔滔, was obtained from The University of Hong Kong (Pokfulam, Hong Kong) and is being sold pursuant to Creative Commons: Attribution 3.0 Hong Kong License. The content of this dissertation has not been altered in any way. We have altered the formatting in order to facilitate the ease of printing and reading of the dissertation. All rights not granted by the above license are retained by the author. Abstract: Abstract of thesis entitled "Anti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II): Thiol "Switch-on" Fluorescent Probes, Thioredoxin Reductase Inhibitors and Endoplasmic Reticulum Targeting Agents" Submitted by ZOU TAOTAO for the degree of Doctor of Philosophy at The University of Hong Kong in Feb 2015 Despite the success of cisplatin in combating various cancers, the problems of resistance and side effects have limited its wide application in cancer treatment. Gold complexes have recently emerged as promising candidates for cancer treatment. Unlike cisplatin, gold complexes do not favor DNA binding, but instead preferentially bind SH/SeH-containing proteins/enzymes in cancer cells, giving hope that these compounds may overcome cisplatin's resistance problems. Since the side effects of cisplatin are, at least partially, caused by instability-associated, off-target binding interactions, the incorporation of N-heterocyclic carbene (NHC) ligands may be a useful strategy to improve the stability of metal-based chemotherapeutics due to the strong donating ability of NHC to form strong M-C(NHC) bonds. Meanwhile, the ease of modification and steric effects of NHC ligands provide favorable lipophilicity, reactivity and binding specificity of metal complexes. Indeed, some Pt(II)-NHC complexes have been reported to specifically target proteins/organelles rather than DNA. 3+ + The reduction of 4-coordinated Au to 2-coordinated Au by thiols has been 3+ demonstrated. Meanwhile, owing to the low energy d 2 2 orbital of Au, most gold(III) x -y complexes are non-emissive in solutions. In Chapter 3, by taking advantage of these unique properties, the synthesis of a class of non-emissive Au(III) complexes containing highly fluorescent N DEGREESN DEGREESN ligands and NHC ligands is described. In these compounds, the NHC ligand prevented further reduction of Au(III) to Au(0) and increased the III + solubility of the Au(III) complexes. The [Au (N DEGREESN DEGREESN)(NHC)] complex was readily reduced by GSH to form [Au (NHC)(GS)], accompanied by the release of the fluorescent H N DEGREESN DEGREESN ligand, therefore acting as a fluorescent "switch-on" probe for thiols. In addition, the anti-cancer activity of Au(I) is owed to its ability to inhibit thiol-enzymes; thus, the Au(III) complexes could also serve as precursors/prodrugs, activated by metal reduction, to deliver anti-cancer active Au(I) species. The major problem of most Au(I) anti-cancer agents is the lack of in vivo anti-tumor activity due to their high thiol-reactivity which leads to many off-target binding interactions with blood thiols. In Chapter 4, the synthesis of a dinuclear gold(I) complex bearing a mixed diphosphine and bis(NHC) ligand is described. This dinuclear Au(I) complex displayed a favorable stability that conveys potent thioredoxin reductase inhibition without being attacked by blood thiols. This complex significantly inhibited tumor growth in two independent mouse models with no observable side effects. The dinuclear Au(I) complex also exhibited anti-angiogenesis activity in a tumor model and inhibited sphere formation of cancer stem cells in vitro. In toxicology studies, neither systemic anaphylaxis in guinea pigs nor localized irritation in rabbits was observed
Book Synopsis Anti-cancer N-heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II) by : 邹滔滔
Download or read book Anti-cancer N-heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II) written by 邹滔滔 and published by . This book was released on 2015 with total page 618 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Anti-cancer N-heterocyclic Carbene Complexes of Platinum(II) and Gold(III) by : 馮善琪
Download or read book Anti-cancer N-heterocyclic Carbene Complexes of Platinum(II) and Gold(III) written by 馮善琪 and published by . This book was released on 2017 with total page 382 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Gold(I) N-heterocyclic Carbene Complexes by : Riccardo Rubbiani
Download or read book Gold(I) N-heterocyclic Carbene Complexes written by Riccardo Rubbiani and published by . This book was released on 2013 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Gold and its Complexes in Anticancer Chemotherapy by : Mohmmad Younus Wani
Download or read book Gold and its Complexes in Anticancer Chemotherapy written by Mohmmad Younus Wani and published by Springer Nature. This book was released on 2021-02-11 with total page 173 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an overview of cancer and the genesis, and development of different treatment strategies and modalities against cancer. The emergence of gold and its complexes as promising anticancer chemotherapeutic agents have the potential to substitute or replace the platinum based chemotherapeutic agents. Gold complexes have demonstrated considerable anti-proliferative properties, chiefly attributed to their anti-mitochondrial effects, they make gold complexes excellent candidates as anti-cancer agents compared to their platinum-based counterparts. This book provides a critical review of recent advances made in the development of gold complexes as anti-cancer agents. In this context, it examines a number of different ligand architectures, provides comprehensive information on gold complexes’ mechanism of action and toxicity issues and, in closing, outlines future research directions.
Book Synopsis Frontiers in Anti-Cancer Drug Discovery, Volume (1) by : Atta-ur- Rahman
Download or read book Frontiers in Anti-Cancer Drug Discovery, Volume (1) written by Atta-ur- Rahman and published by Bentham Science Publishers. This book was released on 2011-02-14 with total page 792 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Frontiers in Anti-Cancer Drug Discovery" is an Ebook series devoted to publishing the latest and the most important advances in Anti-Cancer drug design and discovery. Eminent scientists write contributions on all areas of rational drug design and drug di
Download or read book Medicinal Chemistry written by and published by Academic Press. This book was released on 2020-02-10 with total page 510 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry, Volume 75, the latest release in the Advances in Inorganic Chemistry series, presents timely and informative summaries on current progress in a variety of subject areas. This acclaimed serial features reviews written by experts in the field, serving as an indispensable reference to advanced researchers that empowers readers to pursue new developments in each field. Users will find this to be a comprehensive overview of recent findings and trends from the last decade that covers various kinds of inorganic topics, from theoretical oriented supramolecular chemistry, to the quest for accurate calculations of spin states in transition metals. Provides the authority and expertise of leading contributors from an international board of authors Presents the latest release in the Advances in Inorganic Chemistry series Includes the latest information on medicinal chemistry
Book Synopsis Luminescent and Photoactive Transition Metal Complexes as Biomolecular Probes and Cellular Reagents by : Kenneth Kam-Wing Lo
Download or read book Luminescent and Photoactive Transition Metal Complexes as Biomolecular Probes and Cellular Reagents written by Kenneth Kam-Wing Lo and published by Springer. This book was released on 2015-06-30 with total page 266 pages. Available in PDF, EPUB and Kindle. Book excerpt: The series Structure and Bonding publishes critical reviews on topics of research concerned with chemical structure and bonding. The scope of the series spans the entire Periodic Table and addresses structure and bonding issues associated with all of the elements. It also focuses attention on new and developing areas of modern structural and theoretical chemistry such as nanostructures, molecular electronics, designed molecular solids, surfaces, metal clusters and supramolecular structures. Physical and spectroscopic techniques used to determine, examine and model structures fall within the purview of Structure and Bonding to the extent that the focus is on the scientific results obtained and not on specialist information concerning the techniques themselves. Issues associated with the development of bonding models and generalizations that illuminate the reactivity pathways and rates of chemical processes are also relevant. The individual volumes in the series are thematic. The goal of each volume is to give the reader, whether at a university or in industry, a comprehensive overview of an area where new insights are emerging that are of interest to a larger scientific audience. Thus each review within the volume critically surveys one aspect of that topic and places it within the context of the volume as a whole. The most significant developments of the last 5 to 10 years should be presented using selected examples to illustrate the principles discussed. A description of the physical basis of the experimental techniques that have been used to provide the primary data may also be appropriate, if it has not been covered in detail elsewhere. The coverage need not be exhaustive in data, but should rather be conceptual, concentrating on the new principles being developed that will allow the reader, who is not a specialist in the area covered, to understand the data presented. Discussion of possible future research directions in the area is welcomed. Review articles for the individual volumes are invited by the volume editors. Readership: research scientists at universities or in industry, graduate students Special offer For all customers who have a standing order to the print version of Structure and Bonding, we offer free access to the electronic volumes of the Series published in the current year via SpringerLink.
Book Synopsis Inorganic and Organometallic Transition Metal Complexes with Biological Molecules and Living Cells by : Kenneth Kam-Wing Lo
Download or read book Inorganic and Organometallic Transition Metal Complexes with Biological Molecules and Living Cells written by Kenneth Kam-Wing Lo and published by Academic Press. This book was released on 2016-12-30 with total page 408 pages. Available in PDF, EPUB and Kindle. Book excerpt: Inorganic and Organometallic Transition Metal Complexes with Biological Molecules and Living Cells provides a complete overview of this important research area that is perfect for both newcomers and expert researchers in the field. Through concise chapters written and edited by esteemed experts, this book brings together a comprehensive treatment of the area previously only available through scattered, lengthy review articles in the literature. Advanced topics of research are covered, with particular focus on recent advances in the biological applications of transition metal complexes, including inorganic medicine, enzyme inhibitors, antiparasital agents, and biological imaging reagents. - Geared toward researchers and students who seek an introductory overview of the field, as well as researchers working in advanced areas - Focuses on the interactions of inorganic and organometallic transition metal complexes with biological molecules and live cells - Foscuses on the fundamentals and their potential therapeutic and diagnostic applications - Covers recent biological applications of transition metal complexes, such as anticancer drugs, enzyme inhibitors, bioconjugation agents, chemical biology tools, and bioimaging reagents
Book Synopsis Medicinal Organometallic Chemistry by : Gérard Jaouen
Download or read book Medicinal Organometallic Chemistry written by Gérard Jaouen and published by Springer Science & Business Media. This book was released on 2010-09-14 with total page 305 pages. Available in PDF, EPUB and Kindle. Book excerpt: Contents: Gérard Jaouen, Nils Metzler-Nolte : Introduction ; Stéphane GIBAUD and Gérard JAOUEN: Arsenic - based drugs: from Fowler’s solution to modern anticancer chemotherapy; Ana M. Pizarro, Abraha Habtemariam and Peter J. Sadler : Activation Mechanisms for Organometallic Anticancer Complexes; Angela Casini, Christian G. Hartinger, Alexey A. Nazarov, Paul J. Dyson : Organometallic antitumour agents with alternative modes of action; Elizabeth A. Hillard, Anne Vessières, Gerard Jaouen : Ferrocene functionalized endocrine modulators for the treatment of cancer; Megan Hogan and Matthias Tacke : Titanocenes – Cytotoxic and Anti-Angiogenic Chemotherapy Against Advanced Renal-Cell Cancer; Seann P. Mulcahy and Eric Meggers : Organometallics as Structural Scaffolds for Enzyme Inhibitor Design; Christophe Biot and Daniel Dive : Bioorganometallic Chemistry and Malaria; Nils Metzler-Nolte : Biomedical applications of organometal-peptide conjugates; Roger Alberto : Organometallic Radiopharmaceuticals; Brian E. Mann : Carbon Monoxide – an essential signaling molecule.
Book Synopsis Beyond Cisplatin: N-Heterocyclic Carbene Gold(I) Complexes as Anticancer Agents and Their Use in Drug Delivery Systems by : Jens Oberkofler
Download or read book Beyond Cisplatin: N-Heterocyclic Carbene Gold(I) Complexes as Anticancer Agents and Their Use in Drug Delivery Systems written by Jens Oberkofler and published by . This book was released on 2020 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Synthesis of N-heterocyclic Carbene Gold(I) Complexes by : Luca Boselli
Download or read book Synthesis of N-heterocyclic Carbene Gold(I) Complexes written by Luca Boselli and published by . This book was released on 2014 with total page 158 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biomedical applications of gold complexes based on N-heterocyclic carbenes (NHCs) are beginning to unfold. Some cationic gold(I) NHCs complexes show antimitochondrial activities, a very promising action mode in the fight against cancer; due to their positive charge these complexes target preferentially tumor cells, leading to cell death. In this work of thesis, three groups of new NHC-based gold and heterobimetallic complexes involving aliphatic or aromatic amino-functionalized NHCs with interesting potential in biomedical research have been synthesized and characterized. The first group is formed by three luminescent heterobimetallic gold(I)-ruthenium(II) complexes containing heteroditopic bipyridine-NHC ligands. These compounds have been biologically investigated by in vitro tests for their antitumoral, antileishmanial and antimalarial activities. Finally, imaging studies in cancer cells have been performed exploiting the luminescent properties of the most active compound. The second group of molecules is concerned by cationic gold(I) complexes containing two 1-[2-(diethylamino)ethyl]imidazolydene ligands. First the complexes have been tested for their antiproliferative activity in prostate cancer cell line PC-3. Lipophilicity (Log P) has been determined for these complexes. The most active complex has been tested for the cytotoxic activities in five human cancer cell lines and primary endothelial cells demonstrating a potent action and selectivity for cancer cells. In addition, antileishmanial and antimalarial activities of these compounds have been investigated showing interesting results. The third group is formed by a hetero-dinuclear gold(I)-silver(I) and a trinuclear gold(I)-copper(II) complexes containing phenanthroline-NHC ligands. The compounds are formed by two different organometallic units potentially able to act as multi-targeting anticancer drug.
Book Synopsis Advances in Heterocyclic Chemistry by :
Download or read book Advances in Heterocyclic Chemistry written by and published by Academic Press. This book was released on 2018-05-21 with total page 276 pages. Available in PDF, EPUB and Kindle. Book excerpt: Advances in Heterocyclic Chemistry, Volume 126, is the definitive series in the field, one that is of great importance to organic chemists, polymer chemists and many biological scientists. Because biology and organic chemistry increasingly intersect, the associated nomenclature is used more frequently in explanations. Updates to this release include sections on The Literature of Heterocyclic Chemistry, Part XVI, 2016, The preparation and properties of heteroarylazulenes and hetero-fused azulenes, Recent developments in pyrazole chemistry, Yne, Ene-Yne Synthetic Approaches to Heterocycles, Appel Salt and Heterocycles: A review of Thirty Years of 4,5-Dichloro-1,2,3-dithiazolium Chloride Chemistry, and more. Written by established authorities in the field, this comprehensive review combines descriptive synthetic chemistry and mechanistic insight to yield an understanding on how chemistry drives the preparation and useful properties of heterocyclic compounds. Considered the definitive serial in the field of heterocyclic chemistry Serves as the go-to reference for organic chemists, polymer chemists and many biological scientists Provides timely, comprehensive reviews written by established authorities in the field Combines descriptive synthetic chemistry and mechanistic insight to enhance understanding on how chemistry drives the preparation and useful properties of heterocyclic compounds
Book Synopsis Biomedical Applications of Metals by : Mahendra Rai
Download or read book Biomedical Applications of Metals written by Mahendra Rai and published by Springer. This book was released on 2018-02-24 with total page 332 pages. Available in PDF, EPUB and Kindle. Book excerpt: Focused more specifically on the recent advances in applications of various metals and their complexes used in biomedicine, particularly in the diagnosis and treatment of chronic diseases. The editors give equal importance to other key aspects such as toxicological issues and safety concerns. The application of metals in the biomedical field is highly interdisciplinary and has a broad appeal across all biomedical specialties. Biomedical Applications of Metals is particularly focused on covering the role of metals in medicine and the development of novel therapeutic products and solutions in the form of alternative medicines, and some topics on Indian traditional medicine i.e., “Ayurveda”. In Section I, the book discusses the role of metals in medicines and include chapters on nanoparticles, noble metals, medical devices, copper. selenium, silver, and microbial pathogens; while Section II includes topics on metals toxicity including heavy metals, carcinogens, cancer therapy, Bhasma’s and chelating agents used in Ayurveda, and biochemical and molecular targets including actions of metals. These new and emerging concepts of applications of metals in medicine, their crucial role in management of microbial resistance, and their use in the treatment of various chronic diseases is essential information for toxicologists, and clinical and biomedical researchers.
Book Synopsis Functionalized Platinum (II) and Gold (I) Acetylide Complexes by : Yuen-Ting Shum
Download or read book Functionalized Platinum (II) and Gold (I) Acetylide Complexes written by Yuen-Ting Shum and published by Open Dissertation Press. This book was released on 2017-01-27 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: This dissertation, "Functionalized Platinum (II) and Gold (I) Acetylide Complexes: Structural and Spectroscopic Properties and Anticancer Activities" by Yuen-ting, Shum, 岑婉婷, was obtained from The University of Hong Kong (Pokfulam, Hong Kong) and is being sold pursuant to Creative Commons: Attribution 3.0 Hong Kong License. The content of this dissertation has not been altered in any way. We have altered the formatting in order to facilitate the ease of printing and reading of the dissertation. All rights not granted by the above license are retained by the author. Abstract: Abstract of thesis entitled FUNCTIONALIZED PLATINUM(II) AND GOLD(I) ACETYLIDE COMPLEXES. STRUCTURAL AND SPECTROSCOPIC PROPERTIES AND ANTICANCER ACTIVITIES Submitted by SHUM YUEN TING For the degree of Doctor of Philosophy at The University of Hong Kong in April 2007 Planar [Pt(terpy)X] complexes (terpy = 2,2':6',2''-terpyridine; X = Cl, SR) have frequently been cited as classic DNA metallointercalators in bioinorganic chemistry; + however, application studies of [Pt(terpy)L] (L = monoanionic ligand) and its derivatives in metal-based therapeutics are limited. In this work, a series of platinum(II) terpyridine complexes containing different glycosylated acetylide and arylacetylide ligands were prepared and characterized, the photophysical properties of which were investigated. A low-energy absorption band at 409-476 nm, which was assignable to a MLCT transition was observed in its electronic absorption spectra. Upon photoexcitation, intense emission bands at 513-733 nm were observed and were believed to originate from the excited states of 3 3 MLCT and LLCT character. Cytotoxic activities of the ''Pt(terpy)(glycosylated arylacetylide)'' system with significant inhibitory effect toward a series of carcinoma cell lines were discovered. [Pt( Bu terpy)(L3)](CF SO ) (L3 = 4-ethynylphenoxy 3 3 3 -2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside) (IC = 0.06-0.1 M) was found to be 50 i260-fold more effective in growth inhibition of the human brain cancer cell line (SF-268) than cisplatin. The binding interactions of selected platinum(II) complexes 4 5 -1 3 to calf-thymus DNA featured binding constants of 10-10 mol dm . Significantly, the spectral data were found to support a specific binding mode at the AT sequences of DNA for selected complexes. The results of cytometry experiments showed that [Pt( Bu terpy)(L3)](CF SO ) 3 3 3 induce 52.4% apoptosis in NCI-H460 cells. Based on microarray and Western blotting analyses, down-regulation of anti-apoptotic proteins, including Bcl-2 and caspase-3, were observed for platinum-treated NCI-H460 cells. When taken together, the [Pt( Bu terpy)(L3)](CF SO)-induced apoptosis in NCI-H460 cells should 3 3 3 normally occur via the mitochondrial pathway. A family of mono- and binuclear Cy P-supported gold(I) complexes which contained various π-conjugated arylacetylide ligands, were prepared and characterized. The lowest-energy singlet transitions were predominately intraligand in nature and exhibited both phenyl and acetylenic (ππ*) character. The organic triplet emissions of arylacetylide groups were thus "illuminated" at ambient conditions by ligation to the [Au(PCy )] fragment. Strong photoluminescence was detected in solid and solution states of the gold(I) complexes under ambient conditions with lifetimes in the microsecond regime. Selected gold(I) complexes were also subjected to cytotoxicity analysis; only [Au(PCy )(C≡CC H )] showed cytotoxicities (IC = 3 10 7 50 4.9-14.5 M) that were comparable to clinical cisplatin. An acetylide ligand that was appended with lomefloxacin moiety was coordinated to ii with gold(I) and platinum(II) complexes to form [CyPAu(lome)] and [Pt( Bu tpy)(lome)] (CF SO ) (lome = modified lomefloxacin), both of which were 3 3 3 structurally characterized. Tw
Book Synopsis Metal-based Anticancer Agents by : Angela Casini
Download or read book Metal-based Anticancer Agents written by Angela Casini and published by Royal Society of Chemistry. This book was released on 2019-04-05 with total page 370 pages. Available in PDF, EPUB and Kindle. Book excerpt: Metal-based anticancer drugs are among the most successful therapeutic agents, as evidenced by the frequent prescription of selected platinum and arsenic compounds to patients. Metal-based Anticancer Agents covers the interdisciplinary world of inorganic drug discovery and development by introducing the most prominent compound classes based on different transition metals, discussing emerging concepts and enabling methods, as well as presenting key pre-clinical and clinical aspects. Recent progress on the unique features of next-generation targeted metal-based anticancer agents, including supramolecular coordination complexes used for both therapy and drug delivery, promise a bright future beyond the benefits of pure cytotoxic activity. With contributions from global leaders in the field, this book will serve as a useful reference to established researchers as well as a practical guide to those new to metallodrugs, and postgraduate students of medicinal chemistry and metallobiology.
