Download or read book Synthesis and Anticancer Activity of Long Chain Isonicotinic Ester Ligand Containing Arene Ruthenium Complexes and Nanoparticles written by and published by . This book was released on with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis Nanoparticle Encapsulation and Magnetic Resonance Studies of Metal based Anticancer Complexes written by Gregory MacNeil and published by . This book was released on 2023 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since the discovery of cisplatin, metal complexes continue to gain interest as anticancer agents. Though a breadth of research has been conducted in this field, many pitfalls and questions remain, such as off-target activity and how exactly metal complexes exhibit their activity. In the search for novel complexes that address these issues, ruthenium and copper have become leading choices. Though a vast array of complexes employing these metals have been reported, their clinical development has often been hindered by low activity and a lack in understanding of their mechanism of action. The work in this thesis looks to address these issues in two ways: (i) by developing novel complexes and methods to breath new life into well-studied metal compounds and (ii) employ magnetic resonance spectroscopies to examine their behaviour in relevant biological environments. Chapter 2 discusses the synthesis of a novel Ru(II)-arene complex appended with a selective estrogen receptor modifier to target breast cancer. These novel complexes were subjected to several different cell assays, including the National Cancer Institute NCI-60 screen, which showed increased activity over the inactive parent ruthenium scaffolds. Chapter 3 presents 19F magnetic resonance imaging methods to develop the theranostic applications of a CF3-appended Keppler-type Ru(III) complex. It is shown that these methods can be used to spatially resolve redox and speciation events in tumour tissues, which is important to understanding their mechanism of action. Chapter 4 presents a robust method to encapsulate these CF3 appended Ru(III) anticancer complexes in polymer nanoparticles to increase their aqueous stability. Cell studies revealed an over 10-fold increase in anticancer activity over the free complexes. Chapter 5 presents and in-depth magnetic resonance study of the aqueous solution behaviour of the copper anticancer complex CasIII-ia. EPR and NMR studies were used to characterize Cu species following dissolution in complex solutions containing HSA, and in the presence of whole cells. Finally, Chapter 6 presents a novel Ru(II)-Ru(III) complex combing the unique biological activities of an organometallic Ru(II) RAPTA-type scaffold and a Ru(III) Keppler-type coordination complex. Cytotoxicity studies of the new dinuclear complex show increased activity relative to mononuclear parent compounds.
Download or read book Synthesis of Ru II N6 p cymene Complexes Featuring Biologically Active Co ligands and Their Conjugation to Peptides for Improved Cell Targeting written by Saawan Kumar and published by . This book was released on 2018 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Since cisplatin has been approved by the FDA in 1978, its anticancer capabilities have opened the field to other metals such as ruthenium-based complexes. Although cisplatin is a highly potent anticancer agent, due to its lack of selectivity it results in a number of side effects. Thus, the search to find new anticancer drug delivery mechanisms is equally as important as finding new anticancer drugs. Ruthenium compounds, in particular RuII(arene) ‘piano stool’ complexes with the general formula of [M(arene)(X)(Y)(Z)], have gained a lot of attraction as they have shown to be effective against primary and metastasised tumours. The arene ring creates a hydrophobic area that allows the complex to pass through the cell membrane into the cell, while the ligands X, Y, and Z can be mono- or multi-dentate and can be fine-tuned to modify the chemical and biological properties of the ruthenium complex. The ruthenium complexes synthesised in this project contain a monodentate N-heterocyclic carbene (NHC) and the biologically active bidentate co-ligands 8-hydroxyquinoline (8-HQ) or 2-pyridinecarbothiomamide (PCA). NHC complexes are typically used in catalysis for their strong metal-carbene bond, and NHC complexes have shown to possess potent antiproliferative activity. Privileged structures, such as 8-HQ, can be used as scaffolds with unique biological and intrinsic drug-like properties and these can be conferred upon metal complexation. PCAs act as S,N-bidentate ligands and are gastric mucosal protectants. Upon their complexation to Ru, they have shown potent antiproliferative activity and are acid stable, making them ideal candidates for oral administration. By synthesising Ru complexes with different biologically active ligands, the respective compounds ideally could have multiple or new modes of action, reducing the development of cancer cell resistance. The synthesised complexes were characterised by nuclear magnetic resonance (NMR) spectroscopy, electrospray ionisation (ESI) mass spectrometry, X-ray diffraction (XRD) analysis when possible, and were found to be stable in DMSO and aqueous solutions. With the lack of selectivity of established anticancer agents in mind, targeting peptides were synthesised and the co-ligand ruthenium complexes were conjugated via an NHC linker to the N-terminus of the peptide whilst on solid support. The Ru(8-HQ)-peptide conjugate was synthesised and purified by RP-HPLC in acceptable yields whereas, only trace amounts of the conjugate were obtained for the PCA ligand. The successful conjugation of derivative Ru(8-HQ) to the peptide opens up the path for the synthesis of other metal-peptide conjugates by solid phase chemistry. This offers a alternative path for metal complexes to be targeted to cancer cells improving their efficacy and reducing potential side effects.
Download or read book Synthesis of Ru II 6 p cymene Complexes Featuring Biologically Active Co ligands and Their Conjugation to Peptides for Improved Cell Targeting written by Saawan Kumar and published by . This book was released on 2018 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since cisplatin has been approved by the FDA in 1978, its anticancer capabilities have opened the field to other metals such as ruthenium-based complexes. Although cisplatin is a highly potent anticancer agent, due to its lack of selectivity it results in a number of side effects. Thus, the search to find new anticancer drug delivery mechanisms is equally as important as finding new anticancer drugs. Ruthenium compounds, in particular RuII(arene) 'piano stool' complexes with the general formula of [M(arene)(X)(Y)(Z)], have gained a lot of attraction as they have shown to be effective against primary and metastasised tumours. The arene ring creates a hydrophobic area that allows the complex to pass through the cell membrane into the cell, while the ligands X, Y, and Z can be mono- or multi-dentate and can be fine-tuned to modify the chemical and biological properties of the ruthenium complex. The ruthenium complexes synthesised in this project contain a monodentate N-heterocyclic carbene (NHC) and the biologically active bidentate co-ligands 8-hydroxyquinoline (8-HQ) or 2-pyridinecarbothiomamide (PCA). NHC complexes are typically used in catalysis for their strong metal-carbene bond, and NHC complexes have shown to possess potent antiproliferative activity. Privileged structures, such as 8-HQ, can be used as scaffolds with unique biological and intrinsic drug-like properties and these can be conferred upon metal complexation. PCAs act as S,N-bidentate ligands and are gastric mucosal protectants. Upon their complexation to Ru, they have shown potent antiproliferative activity and are acid stable, making them ideal candidates for oral administration. By synthesising Ru complexes with different biologically active ligands, the respective compounds ideally could have multiple or new modes of action, reducing the development of cancer cell resistance. The synthesised complexes were characterised by nuclear magnetic resonance (NMR) spectroscopy, electrospray ionisation (ESI) mass spectrometry, X-ray diffraction (XRD) analysis when possible, and were found to be stable in DMSO and aqueous solutions. With the lack of selectivity of established anticancer agents in mind, targeting peptides were synthesised and the co-ligand ruthenium complexes were conjugated via an NHC linker to the N-terminus of the peptide whilst on solid support. The Ru(8-HQ)-peptide conjugate was synthesised and purified by RP-HPLC in acceptable yields whereas, only trace amounts of the conjugate were obtained for the PCA ligand. The successful conjugation of derivative Ru(8-HQ) to the peptide opens up the path for the synthesis of other metal-peptide conjugates by solid phase chemistry. This offers a alternative path for metal complexes to be targeted to cancer cells improving their efficacy and reducing potential side effects.
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.
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.
Download or read book Iron Catalysis in Organic Chemistry written by Bernd Plietker and published by John Wiley & Sons. This book was released on 2008-09-08 with total page 295 pages. Available in PDF, EPUB and Kindle. Book excerpt: This first comprehensive book to cover this exciting field also deals with the biological aspects, such as enzymes with iron. Following an introduction, this handy reference and handbook goes on to deal with reductions, oxidations of C, H- and C=C bonds, oxidative allylic oxygenation and amination, the oxidation of heteroatoms, cross coupling reactions, aromatic and nucleophilic substitutions, addition to carbonyl compounds, and cyclisations as well as ring opening reactions. The chapters are clearly classified according to the reaction type, allowing readers to quickly locate the desired information.
Download or read book Quinoxalines written by Vakhid A. Mamedov and published by Springer. This book was released on 2016-04-26 with total page 451 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book reviews the fundamental aspects of quinoxaline chemistry: synthesis, reactions, mechanisms, structure, properties, and uses. The first four chapters present a survey of the developments in quinoxaline chemistry since the publication of the monograph on “Condensed Pyrazines” by Cheeseman and Cookson in 1979. These chapters give comprehensive coverage of all the methods of the synthesis of quinoxalines and the important quinoxaline-containing ring systems such as thiazolo[3,4-a]-, pyrrolo[1,2-a]-, and imidazo[1,5-a]quinoxalines. Chapter five describes many new methods for the construction of quinoxaline macrocycles, which are important in applications such as optical devices and materials. The final chapter reviews all previously known rearrangements of heterocyclic systems that lead to benzimidazole derivatives. Mamedov critically analyses these transformations to reveal a novel acid-catalyzed rearrangement of quinoxalinones giving 2-heteroarylbenzimidazoles and 1-heteroarylbenzimidazolones in the presence of nucleophilic reactants (MAMEDOV Heterocycle Rearrangement). This book is of interest to researchers in the fields of heterocyclic and synthetic organic chemistry.
Download or read book Aqueous Organometallic Catalysis written by Ferenc Joo and published by Springer Science & Business Media. This book was released on 2001-11-30 with total page 307 pages. Available in PDF, EPUB and Kindle. Book excerpt: Over the past 20 years aqueous organometallic catalysis has found applications in small- scale organic synthesis in the laboratory, as well as in the industrial production of chemicals with a combined output close to one million tons per year. Aqueous/organic two-phase reactions allow easy product-catalyst separation and full catalyst recovery which mean clear benefits not only in economic but also in environmental and green chemistry contexts. Instead of putting together a series of expert reviews of specialized fields, this book attempts to give a comprehensive yet comprehensible description of the various catalytic transformations in aqueous systems as seen by an author who has been working on aqueous organometallic catalysis since its origin. Emphasis is put on the discussion of differences between related non-aqueous and aqueous processes due to the presence of water. The book will be of interest to experts and students working in catalysis, inorganic chemistry or organic synthesis, and may serve as a basis for advanced courses.
Download or read book Iron Catalysis written by Bernd Plietker and published by Springer Science & Business Media. This book was released on 2011-01-05 with total page 227 pages. Available in PDF, EPUB and Kindle. Book excerpt: Juan I. Padrón and Víctor S. Martín: Catalysis by means of Fe-based Lewis acids; Hiroshi Nakazawa*, Masumi Itazaki: Fe–H Complexes in Catalysis; Kristin Schröder, Kathrin Junge, Bianca Bitterlich, and Matthias Beller: Fe-catalyzed Oxidation Reactions of Olefins, Alkanes and Alcohols: Involvement of Oxo- and Peroxo Complexes; Chi-Ming Che, Cong-Ying Zhou, Ella Lai-Ming Wong: Catalysis by Fe=X Complexes (X=NR, CR2); René Peters, Daniel F. Fischer and Sascha Jautze: Ferrocene and Half Sandwich Complexes as Catalysts with Iron Participation; Markus Jegelka, Bernd Plietker: Catalysis by Means of Complex Ferrates.
Download or read book Bioorganometallics written by Gérard Jaouen and published by John Wiley & Sons. This book was released on 2006-05-12 with total page 462 pages. Available in PDF, EPUB and Kindle. Book excerpt: This first comprehensive book to cover the expanding field of bioorganometallics represents the perfect starting point for beginners but also an excellent source of high quality information for experts in the field. Edited by a pioneer in the field with an excellent standing within the community, this book begins with the history of bioorganometallics, before going on to cover pharmaceuticals, bioorganometallic chemistry and radiopharmaceuticals. A must for bioinorganic chemists, the pharmaceutical industry, chemists working in organometallics and biochemists.
Download or read book Redox Active Therapeutics written by Ines Batinić-Haberle and published by Springer. This book was released on 2016-10-13 with total page 709 pages. Available in PDF, EPUB and Kindle. Book excerpt: This essential volume comprehensively discusses redox-active therapeutics, focusing particularly on their molecular design, mechanistic, pharmacological and medicinal aspects. The first section of the book describes the basic aspects of the chemistry and biology of redox-active drugs and includes a brief overview of the redox-based pathways involved in cancer and the medical aspects of redox-active drugs, assuming little in the way of prior knowledge. Subsequent sections and chapters describe more specialized aspects of central nervous system injuries, neurodegenerative diseases, pain, radiation injury and radioprotection (such as of brain, lungs, head and neck and erectile function) and neglected diseases (e.g., leishmaniasis). It encompasses several major classes of redox-active experimental therapeutics, which include porphyrins, salens, nitrones, and most notably metal-containing (e.g., Mn, Fe, Cu, Zn, Sb) drugs as either single compounds or formulations with nanomaterials and quantum dots. Numerous illustrations, tables and figures enhance and complement the text; extensive references to relevant literature are also included. Redox-Active Therapeutics is an invaluable addition to Springer’s Oxidative Stress in Applied Basic Research and Clinical Practice series. It is essential reading for researchers, clinicians and graduate students interested in understanding and exploring the Redoxome—the organism redox network—as an emerging frontier in drug design, redox biology and medicine.
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.
Download or read book Metal Complexes in Cancer Chemotherapy written by Bernhard K. Keppler and published by Wiley-VCH. This book was released on 1993-07-01 with total page 434 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents a critical overview of the present status of metal complexes in cancer chemotherapy. Interdisciplinary in approach, the book covers both clinical and experimental aspects of the subject. Topics treated in depth include: - synthesis of metal complexes for cancer chemotherapy - metal complexes in clinical and preclinical trials - the mechanism of action of tumour-inhibiting metal complexes Oncologists and internists as well as researchers and students in organic chemistry, coordination chemistry, biochemistry and biology will find this up-to-date monograph highly valuable in their daily work.
Download or read book Green Approaches in Medicinal Chemistry for Sustainable Drug Design written by Bimal Krishna Banik and published by Elsevier. This book was released on 2024-05-31 with total page 699 pages. Available in PDF, EPUB and Kindle. Book excerpt: Extensive experimentation and high failure rates are a well-recognized downside to the drug discovery process, with the resultant high levels of inefficiency and waste producing a negative environmental impact. Sustainable and Green Approaches in Medicinal Chemistry 2e reveals how medicinal chemistry can play a direct role in addressing this issue. After providing essential context to the growth of green chemistry in relation to drug discovery, the book goes on to identify a broad range of practical techniques and useful insights, revealing how medicinal chemistry techniques can be used to improve efficiency, mitigate failure and increase the environmental benignity of the entire drug discovery process. Drawing on the knowledge of a global team of experts, Sustainable and Green Approaches in Medicinal Chemistry, Second Edition encourages the growth of green medicinal chemistry, and supports medicinal chemists, drug discovery researchers, pharmacologists and all those in related fields across both academia and industry in integrating these approaches into their own work. This second volume of the second edition includes the development of nanoparticles and nanocomposites, as well as the application of ultrasound and microwave-induced methods; studies solventless synthesis; defines the role of steroids; studies reactions in aqueous solution; identifies enzyme-mediated reactions; investigates ionic liquids and deep eutectic solvents; explores natural products; investigates solid supports; realizes the effects of salts; focuses on combinatorial chemistry; develops one-pot methods; analyzes multi-component reactions; investigates dipole moment values; and examines computer-assisted methods. Highlights the need for adoption of sustainable and green chemistry pathways in drug development Reveals risk factors associated with the drug development process and the ways sustainable approaches can help address these Identifies novel and cost effective green medicinal chemistry approaches for improved efficiency and sustainability
Download or read book Structural Phase Transitions written by A. D. Bruce and published by . This book was released on 1981 with total page 344 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book The Chemistry of Contrast Agents in Medical Magnetic Resonance Imaging written by Andre S. Merbach and published by John Wiley & Sons. This book was released on 2013-02-19 with total page 514 pages. Available in PDF, EPUB and Kindle. Book excerpt: Magnetic Resonance Imaging (MRI) is one of the most important tools in clinical diagnostics and biomedical research. The number of MRI scanners operating around the world is estimated to be approximately 20,000, and the development of contrast agents, currently used in about a third of the 50 million clinical MRI examinations performed every year, has largely contributed to this significant achievement. This completely revised and extended second edition: Includes new chapters on targeted, responsive, PARACEST and nanoparticle MRI contrast agents. Covers the basic chemistries, MR physics and the most important techniques used by chemists in the characterization of MRI agents from every angle from synthesis to safety considerations. Is written for all of those involved in the development and application of contrast agents in MRI. Presented in colour, it provides readers with true representation and easy interpretation of the images. A word from the Authors: Twelve years after the first edition published, we are convinced that the chemistry of MRI agents has a bright future. By assembling all important information on the design principles and functioning of magnetic resonance imaging probes, this book intends to be a useful tool for both experts and newcomers in the field. We hope that it helps inspire further work in order to create more efficient and specific imaging probes that will allow materializing the dream of seeing even deeper and better inside the living organisms. Reviews of the First Edition: "...attempts, for the first time, to review the whole spectrum of involved chemical disciplines in this technique..."—Journal of the American Chemical Society "...well balanced in its scope and attention to detail...a valuable addition to the library of MR scientists..."—NMR in Biomedicine
