999C1a:GPP207/12/P625 - Výsledky hledání - Digitální repozitář

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	Novel conformationally locked nucleosides and nucleotides based on bicyclo[3.2.1]octane scaffold as a pseudosugar moiety Šála, Michal ; Dejmek, Milan ; Procházková, Eliška ; Hřebabecký, Hubert ; Rybáček, Jiří ; Dračínský, Martin ; Novák, Pavel ; Rosenbergová, Šárka ; Fukal, J. ; Sychrovský, Vladimír ; Rosenberg, Ivan ; Nencka, Radim A route to a series of novel carbocyclic nucleosides locked in North conformation with bicyclo[3.2.1]octane scaffold was developed. Prepared nucleosides served as a starting material for the synthesis of modified oligomers [d(GCATATCAC), r(GCAUAUCAC), and A9]. Biological effects of the prepared nucleosides as well as the hybridization properties of the appropriate duplexes were evaluated. Úplný záznam
	Enzymatic decomposition of a locked nucleoside phosphoramidate monitored by 31P NMR spectroscopy Procházková, Eliška ; Hřebabecký, Hubert ; Nencka, Radim ; Dračínský, Martin Phosphoramidate derivatives are often used as prodrugs of modified nucleosides. The crucial step for the biologically active compound release in cells is then enzymatic hydrolysis of the phosphoramidate derivative. The enzymatic decomposition of a nucleoside prodrug 1 was monitored using 31P NMR spectroscopy and the structure of the reaction products was determined by 1D and 2D (COSY, HSQC, HMBC) NMR experiments and compared with the products obtained with non-enzymatic hydrolysis of the prodrug. Úplný záznam
	Novel conformationally locked nucleosides and nucleotides Nencka, Radim ; Šála, Michal ; Hřebabecký, Hubert ; Procházková, Eliška ; Mackman, R. ; Barauskas, O. ; Lee, Y. J. ; Tian, Y. We report on a synthesis of two novel types of conformationally locked nucleoside analogues. We prepared 7 membered ring 3’,5’-bridged nucleoside analogs locked in a Southern conformation. These nucleoside analogues were converted in one pot to appropriate phosphoramidate prodrugs using boronate methodology. We also devised and prepared a novel carbocyclic nucleoside by replacing furanose with cyclohexene that resulted in a locked Northern conformation similar to LNA monomers. Further details on the biological activity and application for oligonucleotide synthesis will be discussed in detail. Úplný záznam

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