Redox Active Lipophilic Ruthenium Complexes as Potential Anti-cancer Drugs

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ISBN 13 :
Total Pages : 126 pages
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Book Synopsis Redox Active Lipophilic Ruthenium Complexes as Potential Anti-cancer Drugs by : Nagham Alatrash

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.

Increasing Lipophilicity of Redox Active Ruthenium Complexes as a Means to Enhance Cytotoxicity and Reduce Animal Toxicity

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Book Synopsis Increasing Lipophilicity of Redox Active Ruthenium Complexes as a Means to Enhance Cytotoxicity and Reduce Animal Toxicity by : Nagham Alatrash

Download or read book Increasing Lipophilicity of Redox Active Ruthenium Complexes as a Means to Enhance Cytotoxicity and Reduce Animal Toxicity written by Nagham Alatrash and published by . This book was released on 2012 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: The dinuclear and monomeric ruthenium(II) polypyridyl complexes [(phen)2Ru(tatpp)Ru(phen)2]Cl4 (P) and monomer [(phen)2Ru(tatpp)]Cl2 (MP) are promising candidates for anticancer drug development in terms of the observed anti-tumor activity in mouse models. These complexes contain the redox-active tatpp bridging ligand which seems to be the critical component for biological activity. Ruthenium complexes containing the tatpp ligand have been shown to cleave DNA with an inverse dependence on the [O2], exhibit selective and good cytotoxicity towards a number of cultured malignant cell lines, and have tolerable acute toxicity in mice. Significantly, the animal toxicity of P and MP is significantly less than simple ruthenium polypyridyl complexes, such as [Ru(1,10-phenanthroline)3]2+ which may be due to the enhanced lipophilicity of these complexes. This thesis is a direct test of the following hypothesis. We postulate that by increasing the lipophilicity of P and MP we can further mollify their acute toxicity and enhance their cytotoxicity towards malignant cancer cells. Chapters 1 and 2 of this thesis develop this hypothesis in terms of a review of the prior literature and our synthetic approach to construct such complexes. In Chapter 2, the details of the synthesis and characterization of four new lipophilic ruthenium-tatpp complexes based on the P and MP structures. These are (Ph2phen)2Ru(tatpp)Ru(Ph2phen)2][PF6]4 (PPh2), (Ph2phen, 4,7-diphenyl1-1,10-phenanthroline), [(Me4phen)2Ru(tatpp)Ru(Me4phen)2][PF6]4 (PMe4), (Me4phen, 3,4,7,8 tetramethyl-1,10-phenanthroline), [(Me4phen)2Ru(tatpp)][PF6]2 (MPMe4), [(Ph2phen)2Ru(tatpp)][PF6]2 (MPPh2). All of these can be metathesized to their chloride salt, which is the preferred form for water solubility and biological testing. Chapter 3 presents the effect of these structural changes on the biological activity of the novel complexes in terms of the maximum tolerable dose (MTD) observed in mice, the IC50 values against malignant cell line, H358, and the ability of these complexes to cleave DNA, in vitro. In order to quantify the increase in lipophilicity, the partition coefficients (log P) were determined for the ruthenium complexes via the shake-flask method in PBS at pH 7.4 and octanol as well as in deionized water and octanol. It was found that the lipophilicity of these complexes increased as the lipophilic ancillary ligands changes from phen to Ph2phen and Me4phen ligands. The ability of these complexes to cleave DNA was maintained even with these ligand modifications. The cytotoxicity study against H358 cell line have revealed that the most promising activity was shown by PMe4 and PPh2 with an IC50 value of about 10 [mu]M. The lipophilic ruthenium complexes PPh2, PMe4, MPPh2, MPMe4 showed no acute animal toxicity in a screen of the MTD in Balb/c mice with doses up to 80 mg drug/Kg mouse.

Ruthenium(II) Polypyridyl Complexes as Potential Anticancer Drugs

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Total Pages : pages
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Book Synopsis Ruthenium(II) Polypyridyl Complexes as Potential Anticancer Drugs by : Yanling Chen

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.

Ruthenium Chemistry

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Publisher : CRC Press
ISBN 13 : 1351616501
Total Pages : 386 pages
Book Rating : 4.3/5 (516 download)

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Book Synopsis Ruthenium Chemistry by : Ajay Kumar Mishra

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.

Ruthenium Complexes

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Publisher : John Wiley & Sons
ISBN 13 : 3527695249
Total Pages : 395 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Ruthenium Complexes by : Alvin A. Holder

Download or read book Ruthenium Complexes written by Alvin A. Holder and published by John Wiley & Sons. This book was released on 2017-11-01 with total page 395 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.

Structure-activity Relationships of Ruthenium(II) Polypyridyl Complexes with Redox-active Intercalating Ligands

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ISBN 13 :
Total Pages : 124 pages
Book Rating : 4.:/5 (945 download)

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Book Synopsis Structure-activity Relationships of Ruthenium(II) Polypyridyl Complexes with Redox-active Intercalating Ligands by : Eugenia Soyo Narh

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.

Investigation of Ruthenium (II) Polypyridyl Dimers as Potential Chemotherapeutic Agents

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ISBN 13 : 9780542722615
Total Pages : pages
Book Rating : 4.7/5 (226 download)

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Book Synopsis Investigation of Ruthenium (II) Polypyridyl Dimers as Potential Chemotherapeutic Agents by : Thamara K. Janaratne

Download or read book Investigation of Ruthenium (II) Polypyridyl Dimers as Potential Chemotherapeutic Agents written by Thamara K. Janaratne and published by . This book was released on 2006 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: The exploration of transition metal complexes as chemotherapeutic agents is still a relatively unexplored but promising area of research. Chapter 1 highlights the most successful anticancer drugs and potential drugs based on metal complexes, with an emphasis of platinum and ruthenium complexes. In Chapter 2, the biological activity of a series of novel ruthenium dimers is investigated with special attention given to evaluating their potential as anticancer chemotherapeutic agents. A partial list of the compound prepared includes: [Ru(bpy)(CO)2}2tpphz]4+ (74+), [Ru(bpy)(CH3CN)2}2 tpphz]4+(84+), [Ru(bpy)(C 2O4)}2tpphz] (9), [Ru(bpy)(CO)(Cl)} 2tpphz]2+ (102+), [(bpy) 2Ru(tpphz)Ru(bpy)2]4+ (11 4+), [(phen)2Ru(tpphz)Ru(phen)2] 4+ (124+), [(phen)2Ru(tatpp)Ru(phen) 2]4+ (Pp4+), [(phen) 2Ru(tatpq)Ru(phen)2]4+ (Qp 4+), [(bpy)2Ru(tatpp)Ru(bpy)2]4+ (Pb4+) and [(bpy)2Ru(tatpq)Ru(bpy) 2]4+ (Qb4+). Systematic changes in functions, such as overall charge (+4, +2, 0), the presence or absence of labile ligands, long and short bridging ligands between metal centers, and redox inactive (tpphz) and active (tatpp and tatpq) ligands allowed us to complete a structure-activity evaluation of this class of potential anticancer drugs. Most promising were the cationic dimers containing long, redox active bridging ligands, Pp4, P b4+, Qp4+ and Qb4+, which showed very high DNA binding constants (Kb = 107 to 109 M-1) and good cytotoxicity against cancer cell lines (NSCLC). Animal toxicity studies (mice) showed most cationic complexes to be acutely toxic at relatively lower doses. However, the cationic dimers containing the long tatpp or tatpq bridging ligands were well tolerated in mice with maximum tolerable doses in the range of 67-167 mg/kg for Pp 4+ and 6.7-17 mg/kg for Qp4+ as the chloride salts. These promising results led to a study of the antitumor activity of Pp4+ and Qp 4+ in vivo using a mouse melanoma model. Excitingly, complex Pp4+ seems to inhibit tumor growth in vivo although a little difference in survival times was observed. Nonetheless, the results are promising in that this was an initial screen in which numerous parameters including dosage, frequency of treatment, tumor type, etc., remains unoptimized. The ability of these complexes to damage DNA was evaluated in Chapter 3 by using a plasmid DNA assay that shows if a complex can induce single or double-strand cuts in the DNA molecule. None of the complexes causes any cleavage reactions unless an external reductant is added. However, upon addition of a common biological reductant (glutathione, dithiothritol or ascorbic acid), complex Pp4+ and Qp 4+ could be shown to induce single-strand cuts. Importantly, the DNA cleaving ability of Pp4+ is potentiated under anaerobic conditions, showing that the cleavage is not via O2 activation processes. Further studies established that complex P p4+ is doubly reduced under the assay conditions and the doubly reduced product, denoted H2Pp 4+, is the cleavage agent. As this species is oxygen sensitive and readily reoxidized to Pp4+ upon exposure to air, the [O2] 'regulates' the nuclease activity by controlling [H2Pp4+]. The ability of the ruthenium complexes to inhibit or poison topoisomerase I and II was evaluated and is reported in Chapter 4. The intercalating complexes showed the most significant topoisomerase I and II inhibition with complex Pp4+ standing out again for its potent biological activity.

Iron and Ruthenium Complexes with Nitrogen and Oxygen Donor Ligands for Anti-Cancer and Anti-Viral Studies

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ISBN 13 : 9781361426647
Total Pages : pages
Book Rating : 4.4/5 (266 download)

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Book Synopsis Iron and Ruthenium Complexes with Nitrogen and Oxygen Donor Ligands for Anti-Cancer and Anti-Viral Studies by : LAI-MING ELLA. WONG

Download or read book Iron and Ruthenium Complexes with Nitrogen and Oxygen Donor Ligands for Anti-Cancer and Anti-Viral Studies written by LAI-MING ELLA. WONG and published by . This book was released on 2017-01-27 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: This dissertation, "Iron and Ruthenium Complexes With Nitrogen and Oxygen Donor Ligands for Anti-cancer and Anti-viral Studies" by Lai-Ming, Ella, Wong, 黃禮明, 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 IRON AND RUTHENIUM COMPLEXES WITH NITROGEN AND OXYGEN DONOR LIGANDS FOR ANTI-CANCER AND ANTI-VIRAL STUDIES Submitted by Ella Lai-Ming Wong For the degree of Doctor of Philosophy at The University of Hong Kong in February 2006 Development of drug resistance in cancer chemotherapy has stimulated the search for new anti-cancer drugs. Due to the versatile oxidation states and diverse coordination chemistry, iron and ruthenium compounds are potential candidates for new anti-cancer agents and metallopharmaceuticals. In this study, iron(II) complexes containing polypyridines as auxiliary ligand and ruthenium-oxo oxalato cluster were synthesized and characterized by X-ray crystallography, and their anti-cancer and anti-viral properties were examined. The iron(II) complexes, [Fe(R-qpy)(CH CN) ](ClO ) [qpy = 3 2 4 2 2,2′ 6′,2″ 6″,2′″ 6′″,2″″-quinquepyridine, R = H (1a) and Ph (1b)] and [Fe(Py -OH)(CH CN)](ClO ) (2) [Py-OH = 5 3 4 2 5 2,6-bis[hydroxybis(2-pyridyl)methyl]pyridine] were stable in physiological buffers and exhibited significant cytotoxicities against some established human cancer cell lines. According to the MTT assay, their IC values were 0.1 - 70 50 M; they exhibited more pronounced cytotoxicities against hepatocellular carcinoma cells than against other type of cancer cells. Flow cytometry studies revealed that 1a could cause cell cycle arrest of HeLa cells at the S-phase, which involved DNA synthesis. Complex 1a was found to catalyze epoxidation, aziridination and amidation of hydrocarbons with good substrate conversions and high product yields. The iron(IV)-oxo and -imido reactive intermediates were generated in situ and their formulations were verified by mass spectroscopy. By Evan''s method, the result supported the iron(IV) formulation with a low-spin d electronic configuration (S = 1). A ruthenium-oxo oxalato cluster formulated as Na [Ru ( -O) (C O ) ] (3) 7 4 3 4 2 4 6 was prepared. Structural studies and magnetic measurements revealed that the ruthenium atoms adopted the oxidation states of +III, +III, +III and +IV. Complex 3 showed anti-HIV properties on infected cells. Using the HIV-1(BaL) virus infected Hut/CCR5 cells, 3 was found to exhibit >90% inhibition on viral replication at 5 M concentration. Similar findings were obtained with other HIV-infected cell lines including GHOST/CXCR4 and PBMCs. Complex 3 was non-cytotoxic to these cells even at 50 M concentration. Relevant to anti-HIV activity, 3 was found to inhibit HIV-1 reverse transcriptase activity in vitro with IC = 2 nM. 50 III A series of ruthenium complexes, cis-[Ru (Me -tet)Cl ]ClO [Me -tet = 6 2 4 6 N, N, N′, N′-tetramethyl-3,6-dimethyl-3,6-diazaoctane-1,8-diamine], III III trans-[Ru (pyz) Cl]Cl (pyz = pyrazole), trans-[Ru (3Mepyz) Cl ]Cl 4 2 4 2 II III [3Mepyz = 3-methylpyrazole], [Ru (3Mepyz) ]Cl, [Ru (salen)(H O) ]Y 6 2 2 2 [H-salen = N, N''-bis(salicylidene)ethylenediamine, Y = Cl and PF ], 2 6 III cis-[Ru (cyclen)Cl]Cl [cyclen = 1,4,7,10-tetraazacyclododecane], 2III trans-[Ru (BiIml) Cl]Y [BiIml = biimidazole, Y = Cl and PF], and 2 2 6 II cis-[Ru (BiIml) (DMSO) ](ClO ) were examined for anti-cancer activities. 2 2 4 2 Their IC values were 4 - 100 M and their cytotoxicities could be affected by 50 the auxiliary ligands. The reduction potentials of the ruthenium compounds were +/0 in

Medicinal Organometallic Chemistry

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Publisher : Springer Science & Business Media
ISBN 13 : 3642131840
Total Pages : 305 pages
Book Rating : 4.6/5 (421 download)

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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.

Metal-based Anticancer Agents

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Publisher : Royal Society of Chemistry
ISBN 13 : 1788017676
Total Pages : 370 pages
Book Rating : 4.7/5 (88 download)

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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.

Ruthenium and Other Non-Platinum Metal Complexes in Cancer Chemotherapy

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Publisher : Springer Science & Business Media
ISBN 13 : 3642747604
Total Pages : 228 pages
Book Rating : 4.6/5 (427 download)

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Book Synopsis Ruthenium and Other Non-Platinum Metal Complexes in Cancer Chemotherapy by : Etienne Baulieu

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

Inorganic and Organometallic Transition Metal Complexes with Biological Molecules and Living Cells

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Publisher : Academic Press
ISBN 13 : 012803887X
Total Pages : 408 pages
Book Rating : 4.1/5 (28 download)

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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

Inorganic Chemical Biology

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Publisher : John Wiley & Sons
ISBN 13 : 111851002X
Total Pages : 437 pages
Book Rating : 4.1/5 (185 download)

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Book Synopsis Inorganic Chemical Biology by : Gilles Gasser

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.

Breast Cancer Metastasis and Drug Resistance

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Publisher : Springer Nature
ISBN 13 : 3030203018
Total Pages : 427 pages
Book Rating : 4.0/5 (32 download)

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Book Synopsis Breast Cancer Metastasis and Drug Resistance by : Aamir Ahmad

Download or read book Breast Cancer Metastasis and Drug Resistance written by Aamir Ahmad and published by Springer Nature. This book was released on 2019-08-27 with total page 427 pages. Available in PDF, EPUB and Kindle. Book excerpt: Resistance to therapies, both targeted and systemic, and metastases to distant organs are the underlying causes of breast cancer-associated mortality. The second edition of Breast Cancer Metastasis and Drug Resistance brings together some of the leading experts to comprehensively understand breast cancer: the factors that make it lethal, and current research and clinical progress. This volume covers the following core topics: basic understanding of breast cancer (statistics, epidemiology, racial disparity and heterogeneity), metastasis and drug resistance (bone metastasis, trastuzumab resistance, tamoxifen resistance and novel therapeutic targets, including non-coding RNAs, inflammatory cytokines, cancer stem cells, ubiquitin ligases, tumor microenvironment and signaling pathways such as TRAIL, JAK-STAT and mTOR) and recent developments in the field (epigenetic regulation, microRNAs-mediated regulation, novel therapies and the clinically relevant 3D models). Experts also discuss the advances in laboratory research along with their translational and clinical implications with an overarching goal to improve the diagnosis and prognosis, particularly that of breast cancer patients with advanced disease.

Ligand Design in Medicinal Inorganic Chemistry

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Author :
Publisher : John Wiley & Sons
ISBN 13 : 1118697898
Total Pages : 650 pages
Book Rating : 4.1/5 (186 download)

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Book Synopsis Ligand Design in Medicinal Inorganic Chemistry by : Tim Storr

Download or read book Ligand Design in Medicinal Inorganic Chemistry written by Tim Storr and published by John Wiley & Sons. This book was released on 2014-06-12 with total page 650 pages. Available in PDF, EPUB and Kindle. Book excerpt: Increasing the potency of therapeutic compounds, while limiting side-effects, is a common goal in medicinal chemistry. Ligands that effectively bind metal ions and also include specific features to enhance targeting, reporting, and overall efficacy are driving innovation in areas of disease diagnosis and therapy. Ligand Design in Medicinal Inorganic Chemistry presents the state-of-the-art in ligand design for medicinal inorganic chemistry applications. Each individual chapter describes and explores the application of compounds that either target a disease site, or are activated by a disease-specific biological process. Ligand design is discussed in the following areas: Platinum, Ruthenium, and Gold-containing anticancer agents Emissive metal-based optical probes Metal-based antimalarial agents Metal overload disorders Modulation of metal-protein interactions in neurodegenerative diseases Photoactivatable metal complexes and their use in biology and medicine Radiodiagnostic agents and Magnetic Resonance Imaging (MRI) agents Carbohydrate-containing ligands and Schiff-base ligands in Medicinal Inorganic Chemistry Metalloprotein inhibitors Ligand Design in Medicinal Inorganic Chemistry provides graduate students, industrial chemists and academic researchers with a launching pad for new research in medicinal chemistry.

Bioorganometallics

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Publisher : John Wiley & Sons
ISBN 13 : 3527607110
Total Pages : 462 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Bioorganometallics by : Gérard Jaouen

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.

Biological Inorganic Chemistry

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Publisher : Elsevier
ISBN 13 : 0080556221
Total Pages : 383 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Biological Inorganic Chemistry by : Robert R. Crichton

Download or read book Biological Inorganic Chemistry written by Robert R. Crichton and published by Elsevier. This book was released on 2007-12-11 with total page 383 pages. Available in PDF, EPUB and Kindle. Book excerpt: The importance of metals in biology, the environment and medicine has become increasingly evident over the last twenty five years. The study of the multiple roles of metal ions in biological systems, the rapidly expanding interface between inorganic chemistry and biology constitutes the subject called Biological Inorganic Chemistry. The present text, written by a biochemist, with a long career experience in the field (particularly iron and copper) presents an introduction to this exciting and dynamic field. The book begins with introductory chapters, which together constitute an overview of the concepts, both chemical and biological, which are required to equip the reader for the detailed analysis which follows. Pathways of metal assimilation, storage and transport, as well as metal homeostasis are dealt with next. Thereafter, individual chapters discuss the roles of sodium and potassium, magnesium, calcium, zinc, iron, copper, nickel and cobalt, manganese, and finally molybdenum, vanadium, tungsten and chromium. The final three chapters provide a tantalising view of the roles of metals in brain function, biomineralization and a brief illustration of their importance in both medicine and the environment. Relaxed and agreeable writing style. The reader will not only fiind the book easy to read, the fascinating anecdotes and footnotes will give him pegs to hang important ideas on.Written by a biochemist. Will enable the reader to more readily grasp the biological and clinical relevance of the subject.Many colour illustrations. Enables easier visualization of molecular mechanismsWritten by a single author. Ensures homgeneity of style and effective cross referencing between chapters