Download or read book Ruthenium Polypyridyl Complexes with Anticancer Properties written by Eva Corral Simón and published by . This book was released on 2007 with total page 144 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Ruthenium II Polypyridyl Complexes as Potential Anticancer Drugs written by Yanling Chen and published by . This book was released on 2013 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Research on biological activities of ruthenium polypyridyl complexes (RPCs) continues to attract interest as these complexes have shown promising anticancer activity both in vitro and in vivo.1−3 The mononuclear RPC, [(phen)2Ru(tatpp)]2+ (MP) and related dinuclear complex [(phen)2Ru(tatpp)Ru(phen)2]4+ (P) have been shown to both intercalate with DNA and shown potentiated DNA cleavage under anaerobic and reducing conditions4−5, as well as shown good selectivity and cytotoxicity towards malignant cell lines in vitro and tumors in vivo.5 Both complexes contain the redox-active tatpp ligand which is thought to be an essential component for the observed biological activities. This thesis is focused on developing improvements to the stereoselective syntheses of the chiral complexes, [delta][delta]-P and [delta]-MP. It is also investigated the synthesis of a new analogue [(phen)2Ru(tadbp)]2+ (B) and its chiral form [delta]-B which contains a modified tatpp ligand that is only capable of binding one Ru ion. Moreover this thesis explores the ability of these large complexes to traverse the cell membranes and get into cells and cell nuclei by isolating treated cells and nuclei and determining their ruthenium content by graphite furnace atomic absorption method (GFAAS). The GFAAS data show that the two examined complexes [delta][delta]-P and [delta]-MP are able to quickly penetrate into cancer cells (H-358) and concentrate in nuclei, which is postulated due to their high binding affinity to DNA.

Download or read book Ruthenium Complexes written by Alvin A. Holder and published by John Wiley & Sons. This book was released on 2018-02-27 with total page 344 pages. Available in PDF, EPUB and Kindle. Book excerpt: Edited by a team of highly respected researchers combining their expertise in chemistry, physics, and medicine, this book focuses on the use of rutheniumcontaining complexes in artificial photosynthesis and medicine. Following a brief introduction to the basic coordination chemistry of ruthenium complexes and their synthesis in section one, as well as their photophysical and photochemical properties, the authors discuss in detail the major concepts of artificial photosynthesis and mechanisms of hydrogen production and water oxidation with ruthenium in section two. The third section of the text covers biological properties and important medical applications of ruthenium complexes as therapeutic agents or in diagnostic imaging. Aimed at stimulating research in this active field, this is an invaluable information source for researchers in academia, health research institutes and governmental departments working in the field of organometallic chemistry, green and sustainable chemistry as well as medicine/drug discovery, while equally serving as a useful reference also for scientists in industry.

Download or read book Ruthenium Complexes as Anticancer Agents written by Sreekanth Thota and published by LAP Lambert Academic Publishing. This book was released on 2012-05 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: It could be noted from the literature that the presence of the Ru(II) complexes is found to have anticancer activities. Ruthenium metal is known for a long time. But its discovery as a therapeutic agent has recently. Researchers are focused on the synthesis of ruthenium complexes. Ruthenium has to be incorporated in a complex to make it soluble in body fluids.In the search for anticancer active metal complexes several ruthenium complexes have been reported to be promising as anticancer drugs.Ruthenium also has three main properties that make ruthenium complexes well suited metal for medicinal application. i) Ligand exchange rate, ii) The ability of ruthenium to mimic iron in binding to certain biological molecules. iii) The range of accessible oxidation states. Since tris chelates of ruthenium complexes show intercalative properties with the DNA molecule in-vitro, our main objective was to synthesize several mononuclear ruthenium(II) complexes and evaluate them for in-vitro cytotoxic activity.

Download or read book Advances in Metallodrugs written by Shahid Ul-Islam and published by John Wiley & Sons. This book was released on 2020-07-08 with total page 432 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is organized into 12 important chapters that focus on the progress made by metal-based drugs as anticancer, antibacterial, antiviral, anti-inflammatory, and anti-neurodegenerative agents, as well as highlights the application areas of newly discovered metallodrugs. It can prove beneficial for researchers, investigators and scientists whose work involves inorganic and coordination chemistry, medical science, pharmacy, biotechnology and biomedical engineering.

Download or read book Ruthenium and Other Non Platinum Metal Complexes in Cancer Chemotherapy written by Etienne Baulieu and published by Springer Science & Business Media. This book was released on 2013-03-07 with total page 228 pages. Available in PDF, EPUB and Kindle. Book excerpt: With contributions by numerous experts

Download or read book Ruthenium II Polypyridyl Complexes as Mitochondria targeted Two photon Photodynamic Anticancer Agents written by and published by . This book was released on 2015 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

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 Ruthenium Chemistry written by Ajay Kumar Mishra and published by CRC Press. This book was released on 2018-01-17 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book will describe Ruthenium complexes as chemotherapeutic agent specifically at tumor site. It has been the most challenging task in the area of cancer therapy. Nanoparticles are now emerging as the most effective alternative to traditional chemotherapeutic approach. Nanoparticles have been shown to be useful in this respect. However, in view of organ system complicacies, instead of using nanoparticles as a delivery tool, it will be more appropriate to synthesize a drug of nanoparticle size that can use blood transport mechanism to reach the tumor site and regress cancer. Due to less toxicity and effective bio-distribution, ruthenium (Ru) complexes are of much current interest. Additionally, lumiscent Ru-complexes can be synthesized in nanoparticle size and can be directly traced at tissue level. The book will contain the synthesis, characterization, and applications of various Ruthenium complexes as chemotherapeutic agents. The book will also cover the introduction to chemotherapy, classification of Ru- complexes with respect to their oxidation states and geometry, Ruthenium complexes of nano size: shape and binding- selectivity, binding of ruthenium complexes with DNA, DNA cleavage studies and cytotoxicity. The present book will be more beneficial to researchers, scientists and biomedical. Current book will empower specially to younger generation to create a new world of ruthenium chemistry in material science as well as in medicines. This book will be also beneficial to national/international research laboratories, and academia with interest in the area of coordination chemistry more especially to the Ruthenium compounds and its applications.

Download or read book Redox Active Lipophilic Ruthenium Complexes as Potential Anti cancer Drugs written by Nagham Alatrash and published by . This book was released on 2015 with total page 126 pages. Available in PDF, EPUB and Kindle. Book excerpt: The dinuclear ruthenium(II) polypyridyl complexes (RPCs) [(phen)2Ru(tatpp)Ru(phen)2][PF6]4 (P4+) and the monomeric [(phen)2Ru(tatpp)]Cl2 (MP2+) are promising candidates for anti-cancer drug development in terms of the observed antitumor activity in vivo and in vitro. These complexes contain the redox-active tatpp (9,11,20,22-tetraazatetrapyrido[3,2-a:2'3'-c:3'',2''-1:2''',3''']-pentacene) ligand which seems to be the critical component for biological activity. These complexes cleave DNA when reduced in situ to a radical species. Both complexes exhibit selective cytotoxicity toward cultured malignant cell lines and showed inhibition of tumor growth in vivo. This work expands on this platform by preparing and examining more lipophilic analogues of P4+ and MP2+. Specifically, four lipophilic ruthenium(II) polypyridyl complexes, [(Ph2phen)2Ru(tatpp)Ru(Ph2phen)2][PF6]4 (PPh 4+), (Ph2phen, 4,7-diphenyl-1,10- phenanthroline), [(Me4phen)2Ru(tatpp)Ru(Me4phen)2][PF6]4 (PMe 4+), (Me4phen, 3,4,7,8- tetramethyl-1,10phenanthroline), [(Me4phen)2Ru(tatpp)][PF6]2 (MPMe 2+), and [(Ph2phen)2Ru(tatpp)][PF6]2 (MPPh 2+), have been synthesized and characterized in which 4,7-diphenyl-1,10-phenanthroline or 3,4,7,8-tetramethyl-1,10-phenanthroline ligands were used to replace the 1,10-phenanthroline ligands in P4+ and MP2+. A structure-activity examination of their partition coefficient (log P), DNA cleavage activity, cytotoxicity, and animal acute toxicity followed. Log P data revealed lipophilicity decreased in the order: MPPh 2+ > PPh 4+ > MPMe 2+ > PMe 4+ > MP2+ > P4+ as expected. We hypothesized that increasing the lipophilicity of the ruthenium complexes would increase cytotoxicity and decrease animal toxicity, yet have little effect on their DNA cleavage activity. This is because all four analogues retain the putative DNA cleaving unit (tatpp ligand) but being more lipophilic, they should more easily enter cells, increasing cytotoxicity, and on the same basis, be slower to build up in the bloodstream after IP injection in animal toxicity studies. IC50 values for all complexes were obtained for H358, CCL228, MCF-7, and against normal cell line MCF-10. The cytotoxicity of P4+, MP2+ and [Ru(phen)2dppz]2+ were also evaluated in NSCLC cell lines H358, HCC2450, H522, H1993, H2073, H322, H2122, H460 and the pancreatic cancer (PANC1) cell line using standard MTS and clonogenic assays. The lipophilic ruthenium complexes MPPh 2+, PPh 4+, MPMe 2+, and PMe 4+ showed no acute animal toxicity in a screen of the MTD in Balb/c mice with doses up to 160 mg drug/Kg mouse. Furthermore, the absorption and the distribution of drug after administration by intraperitoneal (IP) injection in male Wister Han rats were discussed. Lastly, we present the results from a NCI-60 panel prescreen of MPPh 2+ complex that was submitted through the Developmental Therapeutics Program of the National Cancer Institute. In comparison with P4+ and MP2+, these analogues generally showed similar DNA cleavage activity, enhanced cytotoxic activity in cultured malignant human cells, and reduced animal toxicity in Balb/c mice.

Download or read book The Effects of the Stereochemistry of Ruthenium II Polypyridyl Complexes on Microtubules as Targets for Chemotherapy written by Radhiyah Himawan and published by . This book was released on 2020 with total page 74 pages. Available in PDF, EPUB and Kindle. Book excerpt: Ruthenium polypyridyl complexes (RPCs) are promising anticancer agents due to their robustness and tunability of their polypyridyl ligands. Their axial chirality generally allows for more selective binding to biological molecules. The ruthenium complexes [Ru(phen)3]Cl2 (RPC 1),[Ru(DIP)3]Cl2 (RPC 2), [(phen)2Ru(tatpp)]Cl2 (RPC 3), [(phen)2Ru(tatpp)Ru(phen)2]Cl4 (RPC 4), and [(phen)2Ru(dppz)]Cl2 (RPC 5) have all been investigated, and RPCs 2, 3, and 4 have shown lower micromolar cytotoxicity against malignant cell lines without irradiation. Here in we show that microtubules (MTs) may be the target of some RPCs in cells and all these RPCs 1-5 promote tubulin polymerization in vitro. How they interact with MTs is still yet to be discovered. We examined how the different enantiomers of RPC 2 and 3 affected the cytotoxicity, the cellular uptake, and the MT polymerization. Chapter 1 of this thesis reviews prior literature and discusses other metal complexes as well as RPCs that have anticancer potential for their cellular target and correlation to their structures. Chapters 2 and 3 presents how the stereochemistry of the RPCs in their chloride salt affects their ability to stabilize MTs in addition to entering the cell in the first place. Chapter 2 also presents evidence that MT stabilization by RPCs may not be simple due to electrostatic interactions. MT stabilization is done by comparing the in vitro polymerization of free tubulin with and without the presence of the microtubule stabilizing agent (MSA) as a factor of increased light scattering at 340 nm. Cellular uptake is done in the non-small cell lung carcinoma cell line, H358. The amount of ruthenium was analyzed using ICP-MS and the protein concentration using a bicinchoninic acid assay and UV-Vis spectrometry. Although there were no significant chiral differences in MT stabilization, there was a difference in cellular uptake of enantiopure RPC 2. Chapter 4 outlines the resolution of the RPCs by use of Na2[As2(+ or -)tartrate2] and Na2[Sb2(+ or -)tartrate2], as well discussing the optimization of the syntheses of Na2[Sb2(+ or -)tartrate2] and K2[Sb2(+ or -)tartrate2].

Download or read book Structure activity Relationships of Ruthenium II Polypyridyl Complexes with Redox active Intercalating Ligands written by Eugenia Soyo Narh and published by . This book was released on 2016 with total page 124 pages. Available in PDF, EPUB and Kindle. Book excerpt: The investigation and development of transition metal complexes as cancer chemotherapeutics has gained a lot of interest in the past few decades and has become a promising area of research. Metal complexes of platinum and ruthenium in particular that have demonstrated success as anticancer drugs or are under exploration currently for clinical use are highlighted in Chapter 1. Chapter 2 describes studies undertaken to understand the neurotoxicity of ruthenium(II) polypyridyl complexes (RPCs), including toxicity in mice and inhibition of the enzyme acetylcholinesterase (AChE), as previous work by Dwyer demonstrated that RPCs could be acutely toxic in mice, presumably due to their inhibition of AChE. Several ruthenium complexes were screened for their enzyme inhibitory potency which was correlated to their structural properties including size, charge, and lipophilicity. In addition, the inhibitory activity of the compounds was correlated to their animal toxicity data so as to understand the potential mode of action of the RPCs in vivo. Chapter 3 describes the synthesis of a series of novel ruthenium(II) polypyridyl complexes and their characterization. These complexes were prepared in an effort to tune the reduction potential of the redox-active intercalating ligand (RAIL) to potentials slightly above and below those observed for the Ru-tatpp complexes. The redox activity of ruthenium-tatpp complexes appears to be responsible for their DNA cleavage activity and these analogues, with slightly different reduction potentials, should give us additional insight into the activity of this class of RPCs. In Chapter 4, the electrochemical properties of the RPCs were measured and correlated with their ability to cause DNA cleavage under reducing conditions with GSH. Complexes with reduction potentials less (more positive) than the redox couple of GSH/GSSG were shown to efficiently cleave DNA. However complexes with higher reduction potentials than the biological reducing agent were not observed to cleave DNA under the same conditions. Cytotoxicity screening of these complexes in human non-small cell lung carcinoma cell lines (NSCLC -- H358 and HOP-62) and breast adenocarcinoma cell line (MCF-7), as well as the non-malignant cell line (MCF-10) was performed and described in Chapter 4.

Download or read book Anticancer Activity of Multinuclear Arene Ruthenium Complexes Coordinated to Dendritic Polypyridyl Scaffolds 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 Metallo Drugs Development and Action of Anticancer Agents written by Astrid Sigel and published by Walter de Gruyter GmbH & Co KG. This book was released on 2018-02-05 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: Volume 18, entitled Metallo-Drugs: Development and Action of Anticancer Agents of the series Metal Ions in Life Sciences centers on biological, medicinal inorganic chemistry. The serendipitous discovery of the antitumor activity of cis-diamminodichloroplatinum(II) (cisplatin) by Barnett Rosenberg in the 1960s is a landmark in metallodrug-based chemotherapy. The success of cisplatin in the clinic, followed by oxaliplatin and carboplatin, along with their drawbacks relating mainly to resistance development and severe toxicity, initiated research on polynuclear platinum complexes and on Pt(IV) complexes as prodrugs. Furthermore, the indicated shortcomings led to the exploration of other transition and main group metal ions, among them Ru(II/III), Au(I/III), Ti(IV), V(IV/V), and Ga(III) including also the essential metal ions Fe(II/III), Cu(I/II), and Zn(II). Ionic as well as covalent and non-covalent interactions between structurally very different complexes and biomolecules like nucleic acids, proteins, and carbohydrates are studied and discussed with regard to their possible anticancer actions. Hence, MILS-18 summarizes the research at the forefront of medicinal inorganic chemistry, including studies on the next-generation, tailor-made anticancer drugs. All this and more is treated in an authoritative and timely manner in the 17 stimulating chapters of this book, written by 39 internationally recognized experts from 10 nations (from the US via Europe to China and Australia). The impact of this vibrant research area is manifested by more than 2700 references, nearly 150 illustrations (more than half in color) and several comprehensive tables. Metallo-Drugs: Development and Action of Anticancer Agents is an essential resource for scientists working in the wide range from enzymology, material sciences, analytical, organic, and inorganic biochemistry all the way through to medicine including the clinic ... not forgetting that it also provides excellent information for teaching.

Download or read book Inorganic Chemical Biology written by Gilles Gasser and published by John Wiley & Sons. This book was released on 2014-06-23 with total page 437 pages. Available in PDF, EPUB and Kindle. Book excerpt: Understanding, identifying and influencing the biological systems are the primary objectives of chemical biology. From this perspective, metal complexes have always been of great assistance to chemical biologists, for example, in structural identification and purification of essential biomolecules, for visualizing cellular organelles or to inhibit specific enzymes. This inorganic side of chemical biology, which continues to receive considerable attention, is referred to as inorganic chemical biology. Inorganic Chemical Biology: Principles, Techniques and Applications provides a comprehensive overview of the current and emerging role of metal complexes in chemical biology. Throughout all of the chapters there is a strong emphasis on fundamental theoretical chemistry and experiments that have been carried out in living cells or organisms. Outlooks for the future applications of metal complexes in chemical biology are also discussed. Topics covered include: • Metal complexes as tools for structural biology • IMAC, AAS, XRF and MS as detection techniques for metals in chemical biology • Cell and organism imaging and probing DNA using metal and metal carbonyl complexes • Detection of metal ions, anions and small molecules using metal complexes • Photo-release of metal ions in living cells • Metal complexes as enzyme inhibitors and catalysts in living cells Written by a team of international experts, Inorganic Chemical Biology: Principles, Techniques and Applications is a must-have for bioinorganic, bioorganometallic and medicinal chemists as well as chemical biologists working in both academia and industry.

Download or read book Anticancer Activity of Some Ruthenium Complexes written by Pankaj Hazarika and published by LAP Lambert Academic Publishing. This book was released on 2014-06-24 with total page 64 pages. Available in PDF, EPUB and Kindle. Book excerpt: Ruthenium complexes are also important as antitumor agents and some are currently under clinical trials. It follows a novel mechanism of action with the prospect of non-cross-resistance, reduced toxicity and acquires different activity. The Ruthenium complexes are suitable towards cisplatin resistance cancer cells, and efficiently exert antitumor action, which may be in part due to the ability of ruthenium complexes to mimic the binding of iron to certain biological molecules that in fact exploits a mechanism for non-toxic transport of iron inside the body. This property is especially attractive for ruthenium complexes. The ability of ruthenium to mimic iron in binding to certain biological molecules make these complexes well suitable for medicinal use, and as an alternative for the platinum anticancer drugs in the treatment of cancer cells, resistant to cisplatin and its analogues. The water soluble Ru complexes are usually suitable for medicinal use, and several Ru based drugs have shown good anticancer activity.The Ru complexes have certain advantages than the platinum complexes due to its solubility in water and low toxicity.

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