Truncated phosphonated C-1′-branched N,O-nucleosides: A new class of antiviral agents
Roberto Romeo,Caterina Carnovale,Salvatore V. Giofrè,Giovanni Romeo,Beatrice Macchi,Caterina Frezza,Francesca Marino-Merlo,Venerando Pistarà,Ugo Chiacchio +8 more
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TLDR
Preliminary biological assays show that β-anomers are able to inhibit HIV in vitro infection at concentrations in the micromolar range and higher SI values with respect to AZT indicated that the compounds were endowed with low cytotoxicity.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2012-06-01 and is currently open access. It has received 25 citations till now.read more
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Isoxazolidine: A Privileged Scaffold for Organic and Medicinal Chemistry
TL;DR: This review aims to be a comprehensive and general summary of the different isoxazolidine syntheses, their use as starting building blocks for the preparation of natural compounds, and their main biological activities.
Journal ArticleDOI
Nucleoside Analogues: Synthesis and Biological Properties of Azanucleoside Derivatives
Dácil Hernández,Alicia Boto +1 more
TL;DR: The azanucleosides are nucleoside analogues where the furanose ring is replaced by a nitrogen-containing ring or chain this article, and their synthesis and their interesting biological properties are discussed in this microreview.
Journal ArticleDOI
Synthesis and biological evaluation of 3-hydroxymethyl-5-(1H-1,2,3-triazol) isoxazolidines.
Roberto Romeo,Salvatore V. Giofrè,Caterina Carnovale,Agata Campisi,Rosalba Parenti,Lorenzo Bandini,Maria A. Chiacchio +6 more
TL;DR: Biological tests show that the synthesized compounds are able to inhibit proliferation of follicular and anaplastic human thyroid cancer cell lines, with IC50 values ranging from 3.87 to 8.76 lM.
Journal ArticleDOI
Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors
Roberto Romeo,Daniela Iannazzo,Lucia Veltri,Bartolo Gabriele,Beatrice Macchi,Caterina Frezza,Francesca Marino-Merlo,Salvatore V. Giofrè +7 more
TL;DR: A series of pyrimidine-2,4-diones linked to an isoxazolidine nucleus have been synthesized and tested as nucleoside analogs, endowed with potential anti-HIV (human immunodeficiency virus) activity.
Journal ArticleDOI
Synthesis and biological properties of 5-(1H-1,2,3-triazol-4-yl)isoxazolidines: a new class of C-nucleosides.
Salvatore V. Giofrè,Roberto Romeo,Caterina Carnovale,Raffaella Mancuso,Santa Cirmi,Michele Navarra,Adriana Garozzo,Maria A. Chiacchio +7 more
TL;DR: A novel series of C-nucleosides, featuring the presence of a 1,2,3-triazole ring linked to an isoxazolidine system, has been designed as mimetics of the pyrimidine nucleobases, and an antiproliferative effect was observed.
References
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Synthesis and absolute configuration of novel N,O-psiconucleosides using (R)-N-phenylpantolactam as a resolution agent.
Pelayo Camps,Tània Gómez,Diego Muñoz-Torrero,Jordi Rull,Laura M. Sanchez,Francesca Boschi,M. Comes‐Franchini,Alfredo Ricci,Teresa Calvet,Mercè Font-Bardia,Erik De Clercq,Lieve Naesens +11 more
TL;DR: A series of novel N,O-psiconucleosides has been prepared in both enantiomeric forms by resolution of an advanced racemic synthetic intermediate using (R)-N-phenylpantolactam as a chiral resolution agent.
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Diastereoselective synthesis of a collection of new homonucleoside mimetics containing pyrrolo[1,2-b]isoxazoline and pyrrolidine rings
TL;DR: The 1,3-dipolar cycloaddition of enantiopure cyclic hydroxylated nitrones and allyl nucleobases has been exploited for the preparation of homonucleoside mimetics, where the furanose ring is replaced by a pyrrolo[1,2-b ]isoxazolidine system as mentioned in this paper.
Journal ArticleDOI
Diastereo- and enantioselective synthesis of 1'-C-branched N,O-nucleosides.
M. G. Saita,Ugo Chiacchio,Daniela Iannazzo,Antonino Corsaro,Pedro Merino,Anna Piperno,T. Previtera,Antonio Rescifina,Giuseppe Romeo,Roberto Romeo +9 more
TL;DR: The asymmetric version of the process exploits the presence of a chiral auxiliary at the carbon atom of nitrone and leads to β-D and β-L nucleosides in good yields.
Journal ArticleDOI
Sur la synthèse des isosérines N-disubstituées à partir des esters α-acétoxy-acryliques
TL;DR: Les isoserines N-disubstituees ont ete preparees selon une nouvelle methode consistant a additionner m e amine aliphatique secondaire sur l'enolacetate du pyruvate d'ethyle, puis a hydrolyser le produit d'addition as discussed by the authors.