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 Pinnasubject
chemistry.chemical_classificationStereochemistryOrganic ChemistryClinical BiochemistryPharmaceutical SciencePyrazoleBiochemistrychemistry.chemical_compoundchemistryDesign synthesisAmideDrug DiscoveryMolecular MedicineMoietyAzoleCarboxylateCytotoxicityMolecular BiologyCarboxylic esterdescription
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.
year | journal | country | edition | language |
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1996-06-01 | Bioorganic & Medicinal Chemistry Letters |