Phosphonated carbocyclic 2'-oxa-3'-aza-nucleosides have been synthesized in good yields by 1,3-dipolar cycloaddition methodology. The cytotoxicity and the reverse transcriptase inhibitory activity of the obtained compounds have been investigated. Phosphonated carbocyclic 2'-oxa-3'-aza-nucleosides, while showing low levels of cytotoxicity, exert a specific inhibitor activity on two different reverse transcriptases, which is comparable with that of AZT, opening new perspectives on their possible use as therapeutic agents, in anti-retroviral and anti-HBV chemotherapy.
Chiacchio, U., Balestrieri, E., Macchi, B., Iannazzo, D., Piperno, A., Rescifina, A., et al. (2005). Synthesis of phosphonated carbocyclic 2 '-oxa-3 '-aza-nucleosides: Novel inhibitors of reverse transcriptase. JOURNAL OF MEDICINAL CHEMISTRY, 48(5), 1389-1394.
Tipologia: | Articolo su rivista |
Citazione: | Chiacchio, U., Balestrieri, E., Macchi, B., Iannazzo, D., Piperno, A., Rescifina, A., et al. (2005). Synthesis of phosphonated carbocyclic 2 '-oxa-3 '-aza-nucleosides: Novel inhibitors of reverse transcriptase. JOURNAL OF MEDICINAL CHEMISTRY, 48(5), 1389-1394. |
IF: | Con Impact Factor ISI |
Lingua: | English |
Settore Scientifico Disciplinare: | Settore BIO/14 Settore CHIM/03 - Chimica Generale e Inorganica |
Revisione (peer review): | Esperti anonimi |
Tipo: | Articolo |
Rilevanza: | Rilevanza internazionale |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm049399i |
Stato di pubblicazione: | Pubblicato |
Data di pubblicazione: | 2005 |
Titolo: | Synthesis of phosphonated carbocyclic 2 '-oxa-3 '-aza-nucleosides: Novel inhibitors of reverse transcriptase |
Autori: | |
Autori: | Chiacchio, U; Balestrieri, E; Macchi, B; Iannazzo, D; Piperno, A; Rescifina, A; Romeo, R; Saglimbeni, M; Sciortino, M; Valveri, V; Mastino, A; Romeo, G |
Appare nelle tipologie: | 01 - Articolo su rivista |
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