Synthesis, cytostatic activity and inhibition of ribonucleotide reductase by 5 '-phosphoramidates and 5 '-diphosphates, of 2 '-O-allyl-arabinofuranosyl nucleosides

Authors
Manfredini, S Baraldi, PG Durini, E Balzarini, J De Clercq, E Karlsson, A Buzzoni, V Thelander, L
Citation
S. Manfredini et al., Synthesis, cytostatic activity and inhibition of ribonucleotide reductase by 5 '-phosphoramidates and 5 '-diphosphates, of 2 '-O-allyl-arabinofuranosyl nucleosides, NUCLEOS NUC, 18(4-5), 1999, pp. 1007-1008
Citations number
5
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES & NUCLEOTIDES
ISSN journal
07328311 → ACNP
Volume
18
Issue
4-5
Year of publication
1999
Pages
1007 - 1008
Database
ISI
SICI code
0732-8311(1999)18:4-5<1007:SCAAIO>2.0.ZU;2-H
Abstract
The diphosphates of a series of 2'-O-allyl-1-beta-D-arabinofuranosyl deriva tives,previously obtained by us, have been prepared and tested for their in hibitory activity in an in vitro assay using R1 and R2 subunits of the puri fied recombinant mouse ribonucleotide reductase (RNR). 2'-O-Allyl-araU diph osphate proved to be inhibitory, with an IC50 of 100 mu M The 5'-phosphoram idate pronucleotide of 2'-O-allyl-araU was also prepared and tested for inh ibition of tumor cell proliferation.