Download or read book Synthesis Characterization and Anticancer Effect of Photoactivatable Ruthenium II Bipyridyl Complexes in Vitro and in Vivo written by Stephanie J. Mehanna and published by . This book was released on 2020 with total page 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 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 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 Synthesis and Characterization of a Photoactivatable Ruthenium II Complex Bearing 2 9 diphenyl 1 10 phenanthroline written by Najwa Mansour and published by . This book was released on 2020 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Ruthenium II Complexes of Mixed Bipyridyl and Dithiolate thiourea Ligands written by Pelokazi Nkombi and published by . This book was released on 2018 with total page 236 pages. Available in PDF, EPUB and Kindle. Book excerpt:
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 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 Synthesis and Structural Characterization of Novel C N benzimidazole Based Ruthenium II Complex with in Vitro Anticancer Activity written by and published by . This book was released on 2021 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Syntheses Characterization and Preliminary Evaluation of Potential Ruthenium Anticancer Complexes Containing Schiff Base Ligands written by Stephen Mensah and published by . This book was released on 2019 with total page 104 pages. Available in PDF, EPUB and Kindle. Book excerpt: Platinum-based drugs have over the years been administered in the treatment of tumours.Unfortunately, platinum resistance and the severe side effects associated with the treatments has necessitated the research for new anti-cancer drugs. Ruthenium(II) and Ruthenium(III) complexes have shown promise as useful alternative anticancer agents. The lead candidates include the Ru(II) complex RAPTA-C, a ruthenium(II)-arene complex [Ru(Îʺ6-p-cymene)Cl2(1,3,5-triaza-7-phosphaadamantane)] and the Ru(III) complex NAMI-A [imidazoleH][trans-Ru(imidazole) (dimethyl sulfoxide)Cl4]. Both compounds have shown potent cytotoxic activity in several primary human tumor models. Unfortunately, NAMI-A could not advance in clinical evaluations due to limited efficacy in vivo, while the clinical evaluation of RAPTA-C is unknown. Therefore, there is a need for novel cancer therapeutics that have high biological activity, are relatively easy to synthesize, and can readily be modified. This work focuses on the use of 2-acetylpyridine and 2-pyridinecarboxaldehyde for the synthesis, characterization, and preliminary evaluation of derivatives of both the RAPTA-C and NAMI-A anticancer complexes containing Schiff base ligands. Here, the results of the synthesis of these compounds and their subsequent characterization using 1H NMR, MS, fluorescence and UV-Vis spectroscopies are presented.
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 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 Synthesis and Characterization of Hybrid Drugs Based on Ruthenium Complex Moiety and Biologically Active Organic Compounds written by Michał Pawel Łomzik and published by . This book was released on 2016 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The main goal of this thesis was synthesis and preliminary characterization of novel ruthenium(II) polypyridyl complexes bearing biologically active molecules as potential theranostic agents. Luminescence for the diagnostic applications, and cytotoxicity for the anticancer, therapeutic applications are considered as the theranostic properties. Four new ligands containing biologically active moieties - 5-(4-4'-methyl-[2,2'-bipyridine]-4-ylbut-1-yn-1-yl)pyridine-2-carbaldehyde semicarbazone (L1), 3-(5-4'-methyl-[2,2'-bipyridine]-4-ylpentyl)imidazolidine-2,4-dione (L2), 5,5-dimethyl-3-(5-4'-methyl-[2,2'-bipyridine]-4-ylpentyl)imidazolidine-2,4-dione (L3) and [1-(5-4'-methyl-[2,2'-bipyridine]-4-ylpentyl)-2,5-dioxoimidazolidin-4-yl]urea (L4) were synthesized and characterized. The ligands were used to obtain nine novel ruthenium(II) polypyridyl complexes. Six complexes were synthesized with ligand L1 ([Ru(bpy)2(L1)]2+, [Ru(Mebpy)2(L1)]2+, [Ru(tBubpy)2(L1)]2+, [Ru(Phbpy)2(L1)]2+, [Ru(dip)2(L1)]2+, [Ru(SO3dip)2(L1)]2-) and three with ligands L2, L3 and L4 ([Ru(bpy)2(L2)]2+, [Ru(bpy)2(L3)]2+, [Ru(bpy)2(L4)]2+) (bpy = 2,2'-bipyridine, Mebpy = 4,4'-dimethyl-2,2-bipyridine, tBubpy = 4,4'-tert-butyl-2,2'-bipyridine, Phbpy = 4,4'-diphenyl-2,2-bipyridine, dip = 4,7-diphenyl-1,10-phenantroline and SO3dip = 4,7-di-(4-sulfonatophenyl)-1,10-phenantroline). The spectroscopic and photophysical properties of those complexes were determined. The presence of ligands L1-L4 in the structure of the complex decreased luminescence quantum yield and luminescence lifetime in comparison with unmodified [Ru(bpy)3]2+ complex. The theoretical calculations have shown that ligands L1-L4 do not have influence on ruthenium core geometry. However, they increased the energy of the HOMO that resulted in a shorter band gap. The simulated electronic absorption spectra were in a good agreement with the experimental data. The interactions between the studied ruthenium complexes and human serum albumin (HSA) were investigated. All studied Ru(II) complexes exhibited strong affinity to HSA with the association constant 105 M-1s-1, which suggests formation of Ru complex-HSA adducts. It was also determined that ruthenium complexes most likely bind to the hydrophobic pocket of protein, located in Sudlow's site I in the subdomain II A. Preliminary cytotoxicity evaluation for the studied ruthenium complexes showed their cytotoxic activity towards cancer cell lines. Those results, together with good luminescence properties of the studied ruthenium complexes (luminescence lifetimes and luminescence quantum yield) make them interesting candidates for potential theranostic applications.
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 Design Synthesis and Characterization of Ruthenium ii and Rhenium i Complexes with Functionalized Ligands for Photo And Electrochemi Luminescence Solvatochromism Molecular Recognition and HPLC Separation Studies written by Meijin Li 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, "Design, Synthesis and Characterization of Ruthenium(II) and Rhenium(I) Complexes With Functionalized Ligands for Photo-and Electrochemi- Luminescence, Solvatochromism, Molecular Recognition and HPLC Separation Studies" by Meijin, Li, 李梅金, 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 DESIGN, SYNTHESIS AND CHARACTERIZATION OF RUTHENIUM(II) AND RHENIUM(I) COMPLEXES WITH FUNCTIONALIZED LIGANDS FOR PHOTO- AND ELECTROCHEMI- LUMINESCENCE, SOLVATOCHROMISM, MOLECULAR RECOGNITION AND HPLC SEPARATION STUDIES Submitted by LI MEIJIN for the degree of Doctor of Philosophy at The University of Hong Kong in July 2006 A series of ruthenium(II) and rhenium(I) diimine complexes containing thia-, selena- and aza-crowns derived from 1,10-phenanthroline, [Ru(bpy) (phen-3S)](ClO ) 2 4 2 (phen-3S = 1,13-dioxa-4,7,10-trithiacyclopentadecano[2,3-f][1,10]phenanthroline), [Ru(bpy) (phen-2S)](ClO ) (phen-2S = 1,7,10,16-tetraoxa-4,13-dithiacyclohexa- 2 4 2 dodecano[2,3-f][1,10]phenanthroline), [Ru(bpy) (phen-S)](ClO ) (phen-S = 1,4,10,13- 2 4 2 tetraoxa-7-thiacyclopentadecano[2,3-f][1,10]phenanthroline), [Ru(bpy) (phen-Se)](ClO ) 2 4 2 (phen-Se = 1,4,10,13-tetraoxa-7-selenacyclopentadecano[2,3-f][1,10]phenanthroline), [Ru(bpy) (phen-OEt](ClO ) (phen-OEt = 5,6-diethoxy-[1,10]phenanthroline), 2 4 2 [Ru(bpy) (phen-2NH)](ClO ) (phen-2NH = 1,13-diaxa-4,7,10-trioxacyclopenta- 2 4 2 decano[2,3-f][1,10]phenanthroline), [Re(CO) (py)(phen-3S)]PF, [Re(CO) (py)(phen-S)]OTf 3 6 3 and [Re(CO) (py)(phen-Se)]OTf have been synthesized and characterized, and their photophysics, electrogenerated chemiluminescence (ECL) and electrochemistry were studied. Their interaction with metal ions was investigated by UV-vis, luminescence, NMR spectroscopy and ECL. [Ru(bpy) (phen-3S)](ClO ) and [Re(CO) (py)(phen-3S)]
Download or read book The Synthesis Characterization and Photophysical Properties of Ruthenium II Bis 4 4 dimethyl 2 2 bypyridine i e Bipyridine bis pyridine and Its Analogues written by David Wilson Wright and published by . This book was released on 1988 with total page 170 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis and Characterization of Cyclometalated Ruthenium II Complexes and Assessment of Their Potential as Pharmaceuticals written by Leslie Ann Morales and published by . This book was released on 2022 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cyclometalated Ruthenium (II) and RAPTA species were synthesized, characterized and evaluated on their photophysical properties and potential as anti-cancer agents. The binding affinity to yeast RNA of one of the newly synthesized compounds containing a thiophene group (LM5400) was compared to its literature precursor (Compound B) containing a phenyl group under gel electrophoresis. Results indicated that the bands of compounds; Compound A, LM3000, Compound B and LM5400 when incubated with yeast RNA, were similar to the control with the expectation of the band of LM5400 being more faint relative to the rest whenever samples were incubated for 24hrs. Photophysical experiments on cyclometalated ruthenium (II) compounds (CompoundA, LM3000, Compound B, LM5400) indicated that these compounds have an absorbance around 360 nm respectively but do not fluoresce due to extremely low emission values. Four hydrolysis studies were done on the cyclometalated ruthenium (II) species under various conditions and monitored via UV/Vis and H-NMR. Underall conditions, the absorbance and the NMR data the complexes with the j6-benzene ring (Compound A and LM3000) changed under aqueous and chloride solutions. In contrast, the absorbance of the complexes with the j6-cymene rings (Compound B and LM5400) only changed upon increased concentration. All compounds synthesized were characterized by NMR. Crystal structures were obtained for newly synthesized compounds, LM3000 and LM5400.
