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Nucleoside-3'-phosphotriesters as key intermediates for the oligoribonucleotide synthesis. III. An improved preparation of nucleoside 3'-phosphotriesters, their 1H NMR characterization and new conditions for removal of 2-cyanoethyl group.

An improved procedure for the transformation of 5'-O-monomethoxytrityl-2'-O-acetyl-3'-phosphates of uridine la, inosine ib and 6-N-benzoyladenosine lc into corresponding 3'/2,2,2-trichloroethyl, 2-cyanoethyl/-phosphates iiaic is reported. H NMR characterization of nucleoside 3'-phosphotriesters is presented. New conditions i.e. anhydrous triethylamine-pyridine treatment have been found for the selective removal of 2-cyanoethyl group from nucleoside 3'-phosphotriesters in the presence of neighbouring 2'-O-acetyl one.

Adenosine

[Fractionation of nucleosides and nucleoside-5'-mono-, di and triphosphates by thin layer chromatography in silufol].

New solvent systems--dioxane--isopropanol--water--ammonium (4:2:4:1) and dioxane--water--ammonium (6:4:1)--for rapid qualitative and quantitative estimation of nucleosides, nucleoside-5'-mono-, di- and triphosphates by thin layer chromatography is Silufol UV-254 are proposed. The Rf values for 40 ribo- and deoxyribonucleotides of these systems are given.

Chromatography, Thin Layer

Changes in the activities of nucleoside triphosphatases and nucleoside kinases in Vero cells infected with Simian virus 40.

Changes in the activities of three enzymes involved in nucleotide metabolism were studied following infection of Vero cells with SV40. The results showed that SV40 infection enhanced the activities of uridine phosphokinase and UMP phosphokinase involved in nucleotide synthesis and suppressed the activity of nucleoside triphosphatases involved in nulceotide degradation. These SV40-induced enzyme activity changes probably served to somehow increase the quantity of nucleotides for virus proliferation.

Animals

[Imidazole nucleosides, III. Nucleosides of 4(5)-aminoimidazole-5(4)-carboxamide (author's transl)].

The synthesis and properties of 13 nucleosides derived from 5-aminoimidazole-4-carboxamide and from 4-aminoimidazole-5-carboxamide are described. The isomers were oriented by comparison of their spectra and colour reactions. All compounds were tested for anticancer activity. 4-Amino-1-(alpha-D-arabinopyranosyl)-imidazole-5-carboxamide significantly inhibits the growth of Ehrlich ascites carcinoma (fluid form) in mice.

Aminoimidazole Carboxamide

1,2,4-Triazole amino nucleosides. 1-beta-D-3'-Amino-3'-deoxyribofuranosyl-1,2,4-triazole-3-carboxamide and related nucleosides.

The synthesis of 1-beta-D-3'-amino-3'-deoxyribofuranosyl-1,2,4-triazole-3-carboxamide--the 3'-amino analogue of ribavirin--and five related nucleoside analogues is described. Each analogue exhibited LD50 concentrations greater than 100 microgram/mL against P-388 mouse lymphoid leukemia cells in tissue culture. Antiviral testing indicated that none of the compounds exhibited significant activity.

Animals