0000000001054146
AUTHOR
R. Bazzanini
Design, synthesis and antiproliferative activity of methyl 4-Iodo-1-β-D-ribofuranosyl-pyrazole-3-carboxylate and related compounds
Abstract In a SAR study on azole-related nucleosides we have designed some pyrazole-nucleoside analogs characterised, for the first time, by a carboxylic ester moiety. 4-Iodo-1-β-D-ribofuranosyl-pyrazole-3-carboxylate showed a wide spectrum of antiproliferative activity and a particularly low cytotoxicity against resting PBL, being, unlike the other azole nucleosides, more active than the corresponding primary amide.
Synthesis and antiproliferative activity of 2'-O-allyl-1-beta-D-arabynofuranosyl-uracil, -cytosine and -adenine
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.