6533b85afe1ef96bd12b8c6a

RESEARCH PRODUCT

Design, synthesis and antiproliferative activity of methyl 4-Iodo-1-β-D-ribofuranosyl-pyrazole-3-carboxylate and related compounds

F. ScintuPier Giovanni BaraldiDonatella LichinoAlessandra PaniSilvia VertuaniDaniele SimoniR. BazzaniniStefano ManfrediniPaolo La CollaElisabetta Pinna

subject

chemistry.chemical_classificationStereochemistryOrganic ChemistryClinical BiochemistryPharmaceutical SciencePyrazoleBiochemistrychemistry.chemical_compoundchemistryDesign synthesisAmideDrug DiscoveryMolecular MedicineMoietyAzoleCarboxylateCytotoxicityMolecular BiologyCarboxylic ester

description

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.

https://doi.org/10.1016/0960-894x(96)00216-8