6533b85bfe1ef96bd12ba9f8
RESEARCH PRODUCT
Synthesis and antiproliferative activity of 2'-O-allyl-1-beta-D-arabynofuranosyl-uracil, -cytosine and -adenine
Jan BalzariniPier Giovanni BaraldiDaniele SimoniStefano ManfrediniErik De ClercqR. Bazzaninisubject
chemistry.chemical_classificationStereochemistryorganic chemicalsOrganic ChemistryClinical Biochemistryfood and beveragesPharmaceutical ScienceUracilBiological activityBiochemistryAdenosineChemical synthesischemistry.chemical_compoundRibonucleotide reductasechemistryBiochemistryDrug DiscoverymedicineMolecular MedicineNucleotideMolecular BiologyNucleosideCytosinemedicine.drugdescription
Abstract With the aim to design potential inhibitors of ribonucleotide reductase (RR), 2′-O-allyl-β-D-arabinofuranosyl-uracil ( 4 ), -cytosine ( 7 ) and -adenosine ( 10 ) were prepared and evaluated for their cytostatic activity against Molt4/C8, CEM and L1210 cell lines. Although our preliminary data do not allow to assess if RR is the intracellular target, the results point to differences in the (anti)metabolic behavior of these compounds. This study also offers a general synthesis of 2′-O-allyl-β-D-arabinofuranosyl nucleosides for potential applications in the preparation of 2′-O-allyl-β-D-oligoarabino nucleotides.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1997-02-01 |