Synthesis and biological evaluation of diastereoisomerically pure N,O-nucleosides |
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| Authors: | Olga Bortolini Antonio De Nino Tommaso Eliseo Riccardo Gavioli Loredana Maiuolo Beatrice Russo Fabio Sforza |
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| Affiliation: | 1. Dipartimento di Chimica, Università della Calabria, Via Bucci 12 C, 87036 Rende (CS), Italy;2. Dipartimento di Scienze e Tecnologie Chimiche, Università di Roma Tor Vergata, Via della Ricerca Scientifica, Roma, Italy;3. Dipartimento di Biochimica e Biologia Molecolare, Università di Ferrara, Via Borsari 46, 44100 Ferrara, Italy |
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| Abstract: | Several N,O-nucleosides have been synthesized in good yields by direct 1,3-dipolar cyclization methodology, in the absence of solvent. A remarkable cis stereoselectivity (de 98%) was observed by tuning the substituents on the nitrone moiety. A good number of these N,O-nucleosides have been evaluated for cytotoxic activity against selected cellular lines. Some of the tested compounds have proven to be potential antiproliferative drugs. |
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