32 research outputs found
Noncovalent RNA-peptide complexes detected by matrix-assisted laser desorption/ionization mass spectrometry
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Stereocontrolled synthesis of the four stereoisomeric diphosphorylphosphonates of carbocyclic 2',3'-dideoxy-2', 3'- didehydro-5'-noradenosine
No full textVerwendung von Pyrimidin- und Purinnucleosiden zur Phrophylaxe und/oder Behandlung von durch Adenoviren verursachten Infekten
No full textChemoenzymatic synthesis of carbocyclic nucleoside analogues with bicyclo[3.1.0]hexyl residues
No full textSynthesis of the four possible stereoisomeric 5'-nor carbocyclic nucleotides from one common enantiomeritally pure starting material
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ChemInform Abstract: Synthesis of the Four Possible Stereoisomeric 5′-Nor Carbocyclic Nucleosides from One Common Enantiomerically Pure Starting Material.
No full textInhibition of hepatitis B virus DNA polymerase by thymidine triphosphate analogues in vitro
No full text A series of thymidine triphosphate analogues was tested for effect inhibitory on DNA polymerase activity in isolated hepatitis B virus (HBV) particles. The most efficient compounds were 2′,3′-dideoxy-3′-fluoro-5-vinyluridine triphosphate [50% inhibititory dose (ID50) = 0.25 μm], 2′,3′-dideoxy-3′-fluoro-5-bromovinyluridine triphosphate (ID50 = 0.80 μm), 2′,3′-dideoxy-3′-fluoro-4-thiothymidine triphosphate (ID50 = 0.80 μm) and 2′,3′-dideoxy-3′-fluoro-5-bromouridine triphosphate (ID50 = 1.00 μm). The inhibitors only moderately influenced the cellular DNA polymerase α (ID50 ranging from 10 μm to 140 μm) but had a noteworthy effect on DNA polymerase β (ID50 ranging from 0.8 μm to 7.0 μm), which could be associated with toxicity and mutagenicity in human cells. Kinetic analysis revealed a competitive type of inhibition for the most efficient compound, fluoro-5-vinyluridine triphosphate. The inhibition constant ( Ki) was estimated to be 0.25 μm compared with a Michaelis constant ( Km) value of about 0.4 μm for the substrate. </jats:p
