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Articles de revues sur le sujet "ANTICANCER METALLODRUG"

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Sullivan, Matthew P., Michael Groessl, Samuel M. Meier, Richard L. Kingston, David C. Goldstone et Christian G. Hartinger. « The metalation of hen egg white lysozyme impacts protein stability as shown by ion mobility mass spectrometry, differential scanning calorimetry, and X-ray crystallography ». Chemical Communications 53, no 30 (2017) : 4246–49. http://dx.doi.org/10.1039/c6cc10150j.

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Hartinger, Christian G., et Bernhard K. Keppler. « CE in anticancer metallodrug research – an update ». ELECTROPHORESIS 28, no 19 (octobre 2007) : 3436–46. http://dx.doi.org/10.1002/elps.200700114.

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Páez-Franco, José C., Miriam R. Zermeño-Ortega, Carmen Myriam de la O-Contreras, Daniel Canseco-González, Jesus R. Parra-Unda, Alcives Avila-Sorrosa, Raúl G. Enríquez, Juan M. Germán-Acacio et David Morales-Morales. « Relevance of Fluorinated Ligands to the Design of Metallodrugs for Their Potential Use in Cancer Treatment ». Pharmaceutics 14, no 2 (11 février 2022) : 402. http://dx.doi.org/10.3390/pharmaceutics14020402.

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Fluorination of pharmaceutical agents has afforded crucial modifications to their pharmacological profiles, leading to important advances in medicinal chemistry. On the other hand, metallodrugs are considered to be valuable candidates in the treatment of several diseases, albeit with the caveat that they may exhibit pharmacological disadvantages, such as poor water solubility, low bioavailability and short circulating time. To surmount these limitations, two approaches have been developed: one based on the design of novel metallodrug-delivering carriers and the other based on optimizing the structure of the ligands bound to the metal center. In this context, fluorination of the ligands may bring beneficial changes (physicochemical and biological) that can help to elude the aforementioned drawbacks. Thus, in this review, we discuss the use of fluorinated ligands in the design of metallodrugs that may exhibit potential anticancer activity.
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Steel, Tasha R., et Christian G. Hartinger. « Metalloproteomics for molecular target identification of protein-binding anticancer metallodrugs ». Metallomics 12, no 11 (2020) : 1627–36. http://dx.doi.org/10.1039/d0mt00196a.

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Doroudian, Maryam, et Jürgen Gailer. « Integrative Metallomics Studies of Toxic Metal(loid) Substances at the Blood Plasma–Red Blood Cell–Organ/Tumor Nexus ». Inorganics 10, no 11 (7 novembre 2022) : 200. http://dx.doi.org/10.3390/inorganics10110200.

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Globally, an estimated 9 million deaths per year are caused by human exposure to environmental pollutants, including toxic metal(loid) species. Since pollution is underestimated in calculations of the global burden of disease, the actual number of pollution-related deaths per year is likely to be substantially greater. Conversely, anticancer metallodrugs are deliberately administered to cancer patients, but their often dose-limiting severe adverse side-effects necessitate the urgent development of more effective metallodrugs that offer fewer off-target effects. What these seemingly unrelated events have in common is our limited understanding of what happens when each of these toxic metal(loid) substances enter the human bloodstream. However, the bioinorganic chemistry that unfolds at the plasma/red blood cell interface is directly implicated in mediating organ/tumor damage and, therefore, is of immediate toxicological and pharmacological relevance. This perspective will provide a brief synopsis of the bioinorganic chemistry of AsIII, Cd2+, Hg2+, CH3Hg+ and the anticancer metallodrug cisplatin in the bloodstream. Probing these processes at near-physiological conditions and integrating the results with biochemical events within organs and/or tumors has the potential to causally link chronic human exposure to toxic metal(loid) species with disease etiology and to translate more novel anticancer metal complexes to clinical studies, which will significantly improve human health in the 21st century.
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Karas, Brittany F., Jordan M. Hotz, Brian M. Gural, Kristin R. Terez, Victoria L. DiBona, Leonor Côrte-Real, Andreia Valente, Brian T. Buckley et Keith R. Cooper. « Anticancer Activity and In Vitro to In Vivo Mechanistic Recapitulation of Novel Ruthenium-Based Metallodrugs in the Zebrafish Model ». Toxicological Sciences 182, no 1 (3 avril 2021) : 29–43. http://dx.doi.org/10.1093/toxsci/kfab041.

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Abstract Ruthenium is popular as a metal core for chemotherapeutics, due to versatile molecular coordination. Because new metallodrugs are synthesized at high rates, our studies included assays in zebrafish to expedite the initial evaluation as anticancer agents. Here we evaluated novel metallodrugs (PMC79 and LCR134), and cisplatin, a widely used platinum-based chemotherapeutic. We hypothesized that this model could characterize anticancer properties and recapitulate previous in vitro results in vivo. Our findings suggest anticancer properties of PMC79 and LCR134 were similar with less toxicity than cisplatin. Exposures from 24 to 72 h at or below the LOAELs of PMC79 and LCR134 (3.9 µM and 13.5 µm, respectively), impaired blood vessel development and tailfin regeneration. Blood vessel examination through live imaging of larvae revealed distinct regional antiangiogenic impacts. The significant decrease in gene expression of the VEGF-HIF pathway and beta-actin could explain the morphological effects observed in the whole organism following exposure. Tailfin amputation in larvae exposed to PMC79 or LCR134 inhibited tissue regrowth and cell division, but did not impact normal cell proliferation unlike cisplatin. This suggests Ru drugs may be more selective in targeting cancerous cells than cisplatin. Additionally, in vitro mechanisms were confirmed. PMC79 disrupted cytoskeleton formation in larvae and P-glycoprotein transporters in vivo was inhibited at low doses which could limit off-target effects of chemotherapeutics. Our results demonstrate the value for using the zebrafish in metallodrug research to evaluate mechanisms and off-target effects. In light of the findings reported in this article, future investigation of PMC79 and LCR134 are warranted in higher vertebrate models.
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Monti, Daria Maria, Domenico Loreto, Ilaria Iacobucci, Giarita Ferraro, Alessandro Pratesi, Luigi D’Elia, Maria Monti et Antonello Merlino. « Protein-Based Delivery Systems for Anticancer Metallodrugs : Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct ». Pharmaceuticals 15, no 4 (30 mars 2022) : 425. http://dx.doi.org/10.3390/ph15040425.

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β-lactoglobulin is the major component of whey. Here, the adduct formed upon the reaction of the protein with oxaliplatin (OXA) has been prepared, structurally characterized by X-ray crystallography and electrospray ionization–mass spectrometry, and evaluated as a cytotoxic agent. The data demonstrate that OXA rapidly binds β-lactoglobulin via coordination with a Met7 side chain upon release of the oxalate ligand. The adduct is significantly more cytotoxic than the free drug and induces apoptosis in cancer cells. Overall, our results suggest that metallodrug/β-lactoglobulin adducts can be used as anticancer agents and that the protein can be used as a metallodrug delivery system.
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Holtkamp, Hannah U., et Christian G. Hartinger. « Advanced metallomics methods in anticancer metallodrug mode of action studies ». TrAC Trends in Analytical Chemistry 104 (juillet 2018) : 110–17. http://dx.doi.org/10.1016/j.trac.2017.09.023.

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Monti, Dara Maria, Giarita Ferraro et Antonello Merlino. « Ferritin-based anticancer metallodrug delivery : Crystallographic, analytical and cytotoxicity studies ». Nanomedicine : Nanotechnology, Biology and Medicine 20 (août 2019) : 101997. http://dx.doi.org/10.1016/j.nano.2019.04.001.

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Artner, Christian, Hannah U. Holtkamp, Wolfgang Kandioller, Christian G. Hartinger, Samuel M. Meier-Menches et Bernhard K. Keppler. « DNA or protein ? Capillary zone electrophoresis–mass spectrometry rapidly elucidates metallodrug binding selectivity ». Chemical Communications 53, no 57 (2017) : 8002–5. http://dx.doi.org/10.1039/c7cc04582d.

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Thèses sur le sujet "ANTICANCER METALLODRUG"

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Boselli, Luca. « Synthesis of N-heterocyclic carbene gold(I) complexes : towards the development of new organometallic drugs ». Toulouse 3, 2014. http://thesesups.ups-tlse.fr/2579/.

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Les applications biomédicales des complexes d'or à base de carbènes N-hétérocycliques (NHC) commencent à se développer. Certains complexes NHCs d'or(I) cationiques montrent une activité antimitochondriale, un mode d'action très prometteur dans la lutte contre le cancer; grâce à leur charge positive ces complexes ciblent préférentiellement les cellules tumorales, conduisant à la mort cellulaire. Dans ces travaux de thèse, trois familles de nouveaux complexes d'or à ligands NHCs et montrant un potentiel intéressant dans le domaine de la recherche biomédicale ont été synthétisés et caractérisés. Le premier groupe est formé par trois composés hétérobimétalliques luminescents or(I)-ruthenium(II) contenant des ligands hétéroditopiques de type bipyridine-NHC. Ces composés ont été étudiés biologiquement par des tests in vitro pour leurs activités antitumorale, antileishmaniale et antipaludique. Enfin, des études d'imagerie par microscopie confocale dans les cellules cancéreuses ont été réalisées en exploitant les propriétés de luminescence de ces composés. Le deuxième groupe est constitué par des complexes d'or(I) contenant deux ligands 1-[2 (diéthylamino)éthyle]imidazolydène. Tout d'abord, ces complexes ont été testés pour leur activité antiproliférative sur une lignée cellulaire du cancer de la prostate PC-3. La lipophilie (Log P) des composés a été déterminée. Le complexe le plus actif a été testé pour son activité cytotoxique sur cinq lignées de cellules tumorales humaines et des cellules endothéliales primaires. Le complexe le plus actif démontré une sélectivité pour les cellules cancéreuses. En outre, les activités anti-leishmaniose et antipaludique des composés ont été étudiées montrant des résultats intéressants. Le troisième groupe concerne un composé hétéro-dinucléaire d'or(I)-argent(I) et un complexe hétéro-trinucléaire or(I)-cuivre(II) contenant des ligands phénantroline-NHC. Ces composés sont formés par deux unités organométalliques différentes, pour une application potentielle en anticancer
Biomedical applications of gold complexes based on N-heterocyclic carbenes (NHCs) are beginning to unfold. Some cationic gold(I) NHCs complexes show antimitochondrial activities, a very promising action mode in the fight against cancer; due to their positive charge these complexes target preferentially tumor cells, leading to cell death. In this work of thesis, three groups of new NHC-based gold and heterobimetallic complexes involving aliphatic or aromatic amino-functionalized NHCs with interesting potential in biomedical research have been synthesized and characterized. The first group is formed by three luminescent heterobimetallic gold(I)-ruthenium(II) complexes containing heteroditopic bipyridine-NHC ligands. These compounds have been biologically investigated by in vitro tests for their antitumoral, antileishmanial and antimalarial activities. Finally, imaging studies in cancer cells have been performed exploiting the luminescent properties of the most active compound. The second group of molecules is concerned by cationic gold(I) complexes containing two 1-[2-(diethylamino)ethyl]imidazolydene ligands. First the complexes have been tested for their antiproliferative activity in prostate cancer cell line PC-3. Lipophilicity (Log P) has been determined for these complexes. The most active complex has been tested for the cytotoxic activities in five human cancer cell lines and primary endothelial cells demonstrating a potent action and selectivity for cancer cells. In addition, antileishmanial and antimalarial activities of these compounds have been investigated showing interesting results. The third group is formed by a hetero-dinuclear gold(I)-silver(I) and a trinuclear gold(I)-copper(II) complexes containing phenanthroline-NHC ligands. The compounds are formed by two different organometallic units potentially able to act as multi-targeting anticancer drug
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Hostetter, Alethia A. 1981. « In vitro and in cellulo interactions of platinum and ruthenium anticancer metallodrugs with RNA ». Thesis, University of Oregon, 2011. http://hdl.handle.net/1794/11254.

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xviii, 125 p. : ill. (some col.)
Since its approval by the FDA in 1978 cisplatin (cis-diamminedichloroplatinum(II)) has revolutionized the treatment of several cancer types, particularly testicular cancer which now has a cure rate greater than 90%. Following the example set by its success, a broad range of antitumor metallodrugs is being developed. One of the most promising of these drugs, currently in Phase Two of clinical trials, is the Ru-based NAMI-A (imadozolium trans -[tetrachloro(dimethylsulfoxide)(imidazole)ruthenate(III)]) which displays low systemic toxicity and strong antimetastatic activity. The majority of anticancer metallodrugs (including NAMI-A and cisplatin) can bind to DNA, which, in many cases, is an important therapeutic target. Much effort has gone into characterizing the DNA binding properties of anticancer metallodrugs. Less study has gone into characterizing the interaction of anticancer mellodrugs with RNA even though RNA is chemically similar to DNA and plays important roles in gene expression and regulation. Focusing on the extensively studied cisplatin, Chapter I covers both what is known about anticancer metallodrug-RNA binding and the information that can be gleaned from DNA binding and drug localization studies. Chapter II provides the details of a kinetic investigation of the in vitro binding of aquated cisplatin to an RNA sequence containing an internal loop derived from the core of the spliceosome, a related RNA hairpin, and the slower reacting DNA hairpin analog. Chapter III follows in cellulo studies with cisplatin-treated S. cerevisiae that demonstrate, using ICP-MS, differences in Pt accumulation in mRNA and rRNA. The effects of cisplatin treatment on S. cerevisiae cell growth and viability were investigated using clonogenic and morphologic assays. In Chapter IV the same protocols were applied in order to investigate Ru accumulation on RNA following S. cerevisiae treatment with NAMI-A. These in cellulo experiments were followed by in vitro binding studies that utilized MALDI-MS to compare Ru interactions with RNA and DNA oligonucleotides following treatment with NAMI-A under different solution conditions, finding enhanced binding in an acidic, reducing environment like that found in tumor tissue. Chapter V pulls together the knowledge gained so far and discusses questions for future investigation. This dissertation includes both previously published and unpublished coauthored material.
Committee in charge: David Tyler, Chairperson; Victoria DeRose, Advisor; Darren Johnson, Member; Andy Berglund, Member; Alice Barkan, Outside Member
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Elena, Michelucci. « MASS SPECTROMETRY AS A TOOL TO STUDY METAL-CONTAINING COMPOUND/PROTEIN INTERACTIONS FOR ANTICANCER METALLODRUG ». Doctoral thesis, 2018. http://hdl.handle.net/2158/1114111.

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Monteiro, Luís Pedro Gomes. « Development of new anticancer metallodrugs ». Master's thesis, 2019. http://hdl.handle.net/10773/28462.

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The success of chemotherapy has been achieved with low molecular weight drugs that have been shown to destroy cancer cells or to control their proliferation. However, there are several side effects associated with the use of many of these drugs, mainly due to the fact that they do not have selectivity, acting on both tumor and non-tumor cells. The use of coordinating compounds (metallo-pharmaceuticals) for anticancer therapy began with the use of platinum compounds, which, despite their well-known severe limitations, are still widely used. These disadvantages led to the need to explore new metallo-pharmaceuticals with different transition metals. Diversified metal ions can lead to complexes with different characteristics, such as geometries or reduction potentials. This flexibility makes them attractive for the development of new therapeutic agents. The use of pre-active drugs as ligands is a good example of how metal compounds can alter/enhance the activity of parent drugs. The present work shows the results of the synthesis and characterization of new metallo-pharmaceuticals of different transition metals, the study of their ability to interact with deoxyribonucleic acid (DNA) and bovine albumin (BSA), as well as their anticancer behaviour.This performance was evaluated by in vitro biological assays, in tumoral and normal breast cell lines, which allowed to measure their anti-tumor capacity and selectivity.
O sucesso da quimioterapia tem sido conseguido à base de fármacos de baixo peso molecular que têm demonstrado capacidade para destruir as células cancerígenas ou para controlar a sua proliferação. No entanto, existem vários efeitos secundários associados ao uso de muitos destes fármacos, maioritariamente devido ao facto de não apresentarem seletividade, isto é, tanto atuarem nas células tumorais como nas não tumorais. O uso de compostos de coordenação (metalofármacos) para terapia anticancerígena começou com o uso de compostos de platina, os quais, apesar das suas bem conhecidas severas limitações, continuam ainda a ser muito utilizados. Estas desvantagens levaram à necessidade de explorar novos metalofármacos com diferentes metais de transição. Iões metálicos diversificados podem levar à obtenção de complexos com características diferentes, como por exemplo, no que diz respeito a geometrias ou potenciais de redução. Esta flexibilidade torna-os atraentes para o desenvolvimento de novos agentes terapêuticos. O uso de fármacos pré-ativos como ligandos é um bom exemplo de como os compostos metálicos podem alterar/melhorar a atividade dos fármacos parentais. O presente trabalho mostra os resultados da síntese e caracterização de novos metalofármacos de diferentes metais de transição, do estudo da sua capacidade de interação com o ácido desoxirribonucleico (ADN) e com a albumina de origem bovina (BSA), bem como do seu comportamento anticancerígeno. Este desempenho foi avaliado através de ensaios biológicos in vitro, em linhas celulares cancerígenas e normais da mama que permitiram aferir da sua capacidade anti-tumoral e seletividade.
Mestrado em Biomedicina Molecular
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Barry, Nicolas P. E., et P. J. Sadler. « 100 years of metal coordination chemistry : from Alfred Werner to anticancer metallodrugs ». 2014. http://hdl.handle.net/10454/11220.

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Alfred Werner was awarded the Nobel Prize in Chemistry just over 100 years ago. We recall briefly the era in which he was working, his co-workers, and the equipment he used in his laboratories. His ideas were ground breaking: not only does a metal ion have a primary valency (“hauptvalenz”, now the oxidation state), but also a secondary valency, the coordination number (“nebenvalenz”). At that time some refused to accept this idea, but he realised that his new thinking would open up new areas of research. Indeed it did. We illustrate this for the emerging field of medicinal metal coordination chemistry, the design of metal-based therapeutic and diagnostic agents. The biological activity of metal complexes depends intimately not only on the metal and its oxidation state, but also on the type and number of coordinated ligands, and the coordination geometry. This provides a rich platform in pharmacological space for structural and electronic diversity. It is necessary to control both the thermodynamics (strengths of metal-ligand bonds) and kinetics of ligand substitution reactions to provide complexes with defined mechanisms of action. Outer-sphere interactions can also play a major role in target recognition. Our current interest is focussed especially on relatively inert metal complexes which were very familiar to Werner (RuII, OsII, RhIII, IrIII, PtII, PtIV).
We thank the Leverhulme Trust (Early Career Fellowship No. ECF-2013-414 to NPEB), the University of Warwick (Grant No. RDF 2013-14 to NPEB) the ERC (Grant No. 247450 to PJS), EPSRC (Grant No. EP/F034210/1) and EC COST Action CM1105 for support.
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Sanghamitra, Nusrat Jahan Mobassarah. « Synthesis, Characterization And Anticancer Activity Of Copper(I) Phosphine Complexes ». Thesis, 2005. http://etd.iisc.ernet.in/handle/2005/1516.

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Soldevila-Barreda, Joan J., Maria Azmanova, Anaïs Pitto-Barry, Patricia A. Cooper, Steven D. Shnyder et Nicolas P. E. Barry. « Preclinical Anticancer Activity of an Electron-Deficient Organoruthenium(II) Complex ». 2020. http://hdl.handle.net/10454/18025.

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Ruthenium compounds have been shown to be promising alternatives to platinum(II) drugs. However, their clinical success depends on achieving mechanisms of action that overcome Pt-resistance mechanisms. Electron-deficient organoruthenium complexes are an understudied class of compounds that exhibit unusual reactivity in solution and might offer novel anticancer mechanisms of action. Here, we evaluate the in vitro and in vivo anticancer properties of the electron-deficient organoruthenium complex [(p-cymene)Ru(maleonitriledithiolate)]. This compound is found to be highly cytotoxic: 5 to 60 times more potent than cisplatin towards ovarian (A2780 and A2780cisR), colon (HCT116 p53+/+ and HCT116 p53−/−), and non-small cell lung H460 cancer cell lines. It shows no cross-resistance and is equally cytotoxic to both A2780 and A2780cisR cell lines. Furthermore, unlike cisplatin, the remarkable in vitro antiproliferative activity of this compound appears to be p53-independent. In vivo evaluation in the hollow-fibre assay across a panel of cancer cell types and subcutaneous H460 non-small cell lung cancer xenograft model hints at the activity of the complex. Although the impressive in vitro data are not fully corroborated by the in vivo follow-up, this work is the first preclinical study of electron-deficient half-sandwich complexes and highlights their promise as anticancer drug candidates.
UF150295/Royal Society; University of Bradford; Government Department of Business, Energy and Industrial Strategy; SBF003\1170/British Heart Foundation Springboard Award; AMS_/Academy of Medical Sciences/United Kingdom
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Azmanova, Maria, Joan J. Soldevila-Barreda, Hani H. Bani, Rianne M. Lord, Anaïs Pitto-Barry, Steven M. Picksley et Nicolas P. E. Barry. « Anticancer activity of electron-deficient metal complexes against colorectal cancer in vitro models ». 2019. http://hdl.handle.net/10454/17321.

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An evaluation of the in vitro cytotoxicity of nine electron-deficient half-sandwich metal complexes towards two colorectal cancer cell lines (HCT116 p53+/+, HCT116 p53-/-) and one normal prostate cell line (PNT2) is presented herein. Three complexes were found to be equally cytotoxic towards both colorectal cancer cell lines, suggesting a p53-independent mechanism of action. These complexes are 12 to 34  more potent than cisplatin against HCT116 p53+/+ and HCT116 p53-/- cells. Furthermore, they were found to exhibit little or no cytotoxicity towards PNT2 normal cells, with selectivity ratios greater than 50. To gain an insight into the potential mechanisms of action of the most active compounds, their effects on the expression levels of a panel of genes were measured using qRT-PCR against treated HCT116 p53+/+ and HCT116 p53-/- cells, and cell cycle analysis was carried out.
The Royal Society grant UF150295, The Academy of Medical Sciences grant SFB003\1170
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Das, Sangeeta. « Ancillary Ligand Effects On The Anticancer Activity Of Ruthenium(II) Piano Stool Complexes ». Thesis, 2009. http://hdl.handle.net/2005/998.

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The thesis “Ancillary Ligand Effects on the Anticancer Activity of Ruthenium (II) Piano Stool Complexes” is an effort to design better antitumor metallodrugs based on ruthenium(II) complexes with various H-bond donor/acceptor ligands and to understand their mechanism of action. Chapter 1 presents a brief review of metallodrugs and their mechanism of action. Different classes of metallodrugs are discussed. A short discussion on ruthenium based anticancer drugs and their established mechanism of action is also included in this chapter. Chapter 2 deals with the synthesis, characterization and anticancer activity of Ru(II) complexes with P(III) and P(V) ligands. The effect of a strong hydrogen bond acceptor on the cytotoxicity of the complexes has been investigated which allows comparison of complexes with ligands possessing a strong hydrogen bond donor or hydrogen bond acceptor. Partial oxidation of the tertiary phosphine ligands leads to a decrease in cytotoxicity of the ligand, while coordination to ruthenium resulted in a significant increase in the cytotoxicity. A molecular mechanism of action for these complexes was suggested on the basis of various biophysical studies. These complexes bind DNA through non-intercalative interactions which lead to the destabilization of the double helix of the DNA and also unwinding of the negatively supercoiled DNA. Results show that the presence of a hydrogen bond acceptor on the ligand is not capable of enhancing interactions with DNA in comparison with hydrogen bond donor groups. Cellular studies of these complexes showed that inhibition of DNA synthesis and apoptosis occur on treatment with these complexes. Interestingly, these complexes are found to be not only cytotoxic but also antimetastatic. Chapter 3 deals with the synthesis, characterization and anticancer activity of Ru(II) complexes with biologically active S containing heterocyclic ligands and their mechanistic study. Complexation of ruthenium with mercaptobenzothiazole (MBT) gave the most cytotoxic complex (H3) in the series. Heterocyclic Ru(II) complexes behave differently as evidenced by cellular and biophysical studies. Unlike phosphine complexes, H3 shows biphasic melting of DNA at higher concentrations which suggests two different types of interaction with DNA. Chapter 4 deals with synthesis and characterization of water soluble multiruthenated hydrophilic ruthenium(II) complexes with urotropine. An increase in cytotoxicity and binding affinity has been observed with increase in the number of ruthenium atoms per molecule. The complex with three ruthenium atoms showed the best activity. However cytotoxicity of the complexes decreases with decrease in the lipophilicity of the complexes. Chapter 5 describes studies on the interaction of Ru complexes with water, ss-DNA, AMP, GMP and GSH by various spectroscopic techniques. Hydrolysis of Ru-Cl bond in the complexes correlates with the cytotoxicity. Chapter 6 reports the summary of the observations of the thesis and the future prospects of metallodrugs.
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Habas, Khaled S. A., Barreda Joan J. Soldevila, Maria Azmanova, Laia Rafols, Anaïs Pitto-Barry, Diana Anderson et Nicolas P. E. Barry. « Evaluation of the toxicity of two electron-deficient half-sandwich complexes against human lymphocytes from healthy individuals ». 2020. http://hdl.handle.net/10454/18162.

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Electron‐deficient half‐sandwich complexes are a class of under‐studied organometallics with demonstrated potential as metallodrug candidates. The present study investigates the effect of two 16‐electron organoruthenium complexes ([( p‐ cym)Ru(benzene‐1,2‐dithiolato)] ( 1 ) and [( p ‐cym)Ru(maleonitriledithiolate)] ( 2 )) on the cell viability of non‐immortalised human lymphocytes from healthy individuals. The genotoxic effects of 1 and 2 in lymphocytes using the Comet and cytokinesis‐block micronucleus assays is also investigated. Gene expression studies were carried out on a panel of genes involved in apoptosis and DNA damage repair response. Results show that the two 16‐electron complexes do not have significant effect on the cell viability of human lymphocytes from healthy individuals. However, an increase in DNA damage is induced by both compounds, presumably through oxidative stress production.
This project was supported by the Royal Society (University Research Fellowship No. UF150295 to NPEB), the University of Bradford (RDF Award), and by the Academy of Medical Sciences/the Wellcome Trust/ the Government Department of Business, Energy and Industrial Strategy/ the British Heart Foundation Springboard Award [SBF003\1170 to NPEB].
The full-text of this article will be released for public view at the end of the publisher embargo on 30 Oct 2021.
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Livres sur le sujet "ANTICANCER METALLODRUG"

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Unconventional Anticancer Metallodrugs and Strategies to Improve their Pharmacological Profile. MDPI, 2019. http://dx.doi.org/10.3390/books978-3-03921-316-0.

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Chapitres de livres sur le sujet "ANTICANCER METALLODRUG"

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Mejía, Carmen, Said Ortega-Rosales et Lena Ruiz-Azuara. « Mechanism of Action of Anticancer Metallodrugs ». Dans Biomedical Applications of Metals, 213–34. Cham : Springer International Publishing, 2018. http://dx.doi.org/10.1007/978-3-319-74814-6_10.

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Sullivan, Matthew P., Hannah U. Holtkamp et Christian G. Hartinger. « 13. Antitumor Metallodrugs that Target Proteins ». Dans Metallo-Drugs : Development and Action of Anticancer Agents, sous la direction de Astrid Sigel, Helmut Sigel, Eva Freisinger et Roland K. O. Sigel, 351–86. Berlin, Boston : De Gruyter, 2018. http://dx.doi.org/10.1515/9783110470734-019.

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Pötsch, Isabella, Dina Baier, Bernhard K. Keppler et Walter Berger. « CHAPTER 12. Challenges and Chances in the Preclinical to Clinical Translation of Anticancer Metallodrugs ». Dans Metal-based Anticancer Agents, 308–47. Cambridge : Royal Society of Chemistry, 2019. http://dx.doi.org/10.1039/9781788016452-00308.

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« Anticancer Metallodrugs ». Dans Encyclopedia of Metalloproteins, 74. New York, NY : Springer New York, 2013. http://dx.doi.org/10.1007/978-1-4614-1533-6_100080.

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« Detoxification of Anticancer Metallodrugs ». Dans Encyclopedia of Metalloproteins, 756. New York, NY : Springer New York, 2013. http://dx.doi.org/10.1007/978-1-4614-1533-6_100426.

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Uivarosi, Valentina, et Alexandra‐Cristina Munteanu. « Flavonoid Complexes as Promising Anticancer Metallodrugs ». Dans Flavonoids - From Biosynthesis to Human Health. InTech, 2017. http://dx.doi.org/10.5772/67879.

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« 13. ANTITUMOR METALLODRUGS THAT TARGET PROTEINS ». Dans Metallo-Drugs : Development and Action of Anticancer Agents, 351–86. De Gruyter, 2018. http://dx.doi.org/10.1515/9783110470734-013.

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« 7. MEDICINAL CHEMISTRY OF GOLD ANTICANCER METALLODRUGS ». Dans Metallo-Drugs : Development and Action of Anticancer Agents, 199–218. De Gruyter, 2018. http://dx.doi.org/10.1515/9783110470734-007.

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Valente, Andreia, Tânia S. Morais, Ricardo G. Teixeira, Cristina P. Matos, Ana Isabel Tomaz et M. Helena Garcia. « Ruthenium and iron metallodrugs : new inorganic and organometallic complexes as prospective anticancer agents ». Dans Synthetic Inorganic Chemistry, 223–76. Elsevier, 2021. http://dx.doi.org/10.1016/b978-0-12-818429-5.00010-7.

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Actes de conférences sur le sujet "ANTICANCER METALLODRUG"

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Ferraro, Giarita, Alessandro Pratesi, Denana Miodragovic, Paola Imbimbo, Daria Monti, Thomas O' Halloran, Luigi Messori et Antonello Merlino. « Ferritin-based anticancer metallodrug delivery : Encapsulation of Arsenoplatin-1 within the ferritin nanocage ». Dans 6th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland : MDPI, 2020. http://dx.doi.org/10.3390/ecmc2020-07415.

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