Synthesis, cytostatic activity and inhibition of ribonucleotide reductase by 5'-phosphoramidates and 5'-diphosphates, of 2'-O-allyl- arabinofuranosyl nucleosides
| Autor: | E. De Clercq, V. Buzzoni, Elisa Durini, L. Thelander, Jan Balzarini, P. G. Baraldi, Anna Karlsson, Stefano Manfredini |
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| Jazyk: | angličtina |
| Rok vydání: | 1999 |
| Předmět: |
Cell division
Stereochemistry Chemistry organic chemicals food and beverages Tumor cells Antineoplastic Agents Nucleosides Inhibitory postsynaptic potential Biochemistry In vitro law.invention Mice Ribonucleotide reductase Organophosphorus Compounds law Ribonucleotide Reductases Genetics Recombinant DNA Animals Enzyme Inhibitors IC50 Cell Division |
| Zdroj: | Scopus-Elsevier |
| Popis: | The diphosphates of a series of 2′-O-allyl-1-β-D-arabinofuranosyl derivatives, previously obtained by us, have been prepared and tested for their inhibitory activity in an in vitro assay using R1 and R2 subunits of the purified recombinant mouse ribonucleotide reductase (RNR). 2′-O-Allyl-araU diphosphate proved to be inhibitory, with an IC50 of 100 μM. The 5′-phosphoramidate pronucleotide of 2′-O-allyl-araU was also prepared and tested for inhibition of tumor cell proliferation. |
| Databáze: | OpenAIRE |
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