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Nové modifikované nukleosidy s protivirovou nebo cytostatickou aktivitou / Novel modified nucleosides with antiviral or cytostatic activityTokarenko, Anna January 2021 (has links)
A general and modular synthetic approach to 4-substituted phenyl, 2-substituted pyridin- 5-yl and 5-substituted pyridin-2-yl 2′-C-methyl-C-ribonucleosides as potential anti-HCV agents was developed. Addition of halo(het)aryllithium reagents to benzylated 2-C-methyl-D- ribonolactone gave the corresponding hemiketals, which were subsequently converted to the β-anomeric benzyl-protected bromo(het)aryl-C-nucleosides via either direct reduction (in the case of phenyl derivative) or acetylation followed by reduction of the resulting hemiketal acetates (in the case of pyridyl derivatives). The key halogenated (het)aryl-C-nucleoside intermediates were further transformed by Pd-catalyzed cross-coupling, hydroxylation and amination reactions affording series of protected C-nucleosides with small hydrophilic and hydrophobic substituents. The final protecting group removal was rather problematic, and different debenzylation methods, such as hydrogenation on Pd/C or treatment with BCl3, had to be optimized for each derivative to minimize the formation of side-products. The final C- nucleosides were also converted into their 5′-O-triphosphates, and biological activity screenings revealed that none of the free C-nucleosides possesses any antiviral activity in the HCV replicon assay, and none of their NTPs...
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Podjednotka delta bakteriální RNA polymerázy a její role v regulaci genové exprese u Bacillus subtilis / delta subunit of bacterial RNA pol and its role in regulation of gene expression in B. subtilisDvořáček, Lukáš January 2010 (has links)
Delta subunit of bacterial RNA pol and its role in regulation of gene expression in B. subtilis. In this work I focus on regulation of eubacterial gene expression. First, I describe recent knowledge about a key stage of gene expression - transcription, focusing on regulation of trancription iniciation via small effector molecules (guanosine tetraphosphate, initiating nucleoside triphosphate) that are important for the regulation of ribosomal RNA. Second, in the experimental part of my work, I focus on the role of the _ protein, a subunit of RNA polymarase in gram positive bacteria, in transcription iniciation and its effects on regulation of RNA polymerase by the concentration of initiating nucleoside triphosphates.
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Identifizierung von Biomarkern für die Prognose der Gemcitabin-Therapie beim Pankreaskarzinom: RNA-, DNA- und Immunhistochemische- Analysen / Identification of biomarkers for the prognosis in gemcitabine treated pancreatic cancer: RNA-, DNA- and immunhistochemical- analysisZimmer, Christian 11 February 2015 (has links)
No description available.
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Funktionelle und genetische Variabilität bei der zytotoxischen Wirkung von Nukleosid-Analoga / Functional and genetic variability in the cytotoxic action of nucleosid analoguesKuschel, Christian 16 May 2012 (has links)
No description available.
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The kinase MK2 in DNA replication upon genotoxic stress and chemotherapy / Die Kinase MK2 in der DNA-Replikation nach genotoxischem Stress und ChemotherapieKöpper, Frederik 17 October 2012 (has links)
No description available.
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Studium redoxních reakcí a adsorpce 4-nitrofenyltriazolem značených nukleosidů a kresolů na borem dopovaných diamantových elektrodách pro vývoj elektroanalytických metod / Study of redox reactions and adsorption of 4-nitrophenyl triazole labeled nucleosides and cresols on boron doped diamond electrodes for development of electroanalytical methodsVosáhlová, Jana January 2020 (has links)
In this work, the application of boron-doped diamond electrodes with various surface pre- treatment were tested on selected oxidizable and reducible model compounds, specifically para and ortho cresols and 2'-deoxycytidine and 7-deazaadenosine labeled by 4-nitrophenyl triazole. The aim of the study was the investigation of electrochemical and adsorptive processes with respect to the development of electroanalytical methods of detection of the selected compounds, or utilization of boron-doped diamond electrodes as detectors in liquid-flow systems. Cresols were used as the model oxidizable compound. On O-terminated and polished boron- doped diamond electrodes, cresols provide oxidation signal owing to their oxidation to methylphenoxy radical at comparable potentials as on other carbon-based electrodes used as a reference in this work, i.e., glassy carbon electrode, pyrolytic graphite electrode, and carbon paste electrode. These carbon electrode materials show relatively high propensity to adsorption of reaction products, while such adsorption is minimal on boron-doped diamond. In situ anodic activation allows for a rapid regeneration of boron-doped diamond surface prior to each scan. A differential pulse voltammetric method that was developed with a detection limit of 0.61 mol∙l-1 to 2.97 mol∙l-1...
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