Synthesis and biological evaluation of 3-hydroxymethyl-5-(1H-1,2,3-triazol) isoxazolidines |
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| Authors: | Roberto Romeo Salvatore V Giofrè Caterina Carnovale Agata Campisi Rosalba Parenti Lorenzo Bandini Maria A Chiacchio |
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| Institution: | 1. Dipartimento di Scienze del farmaco e dei prodotti per la salute, Via SS Annunziata, 98168 Messina, Italy;2. Dipartimento di Scienze del Farmaco, Via A. Doria 6, 95125 Catania, Italy;3. Dipartimento di Scienze Bio-Mediche, Sezione di Fisiologia, Via A. Doria 6, 95125 Catania, Italy;4. Dipartimento G.F. Ingrassia, Istituto di Igiene e Sanità Pubblica, Via S. Sofia 87, 95123 Catania, Italy |
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| Abstract: | A synthetic approach towards a series of 3-hydroxymethyl-5-(1H-1,2,3-triazol)isoxazolidines has been reported, according to a procedure based on the cycloaddition reaction, under microwave irradiation, of a nitrone with 1-vinyl triazoles, prepared by a click reaction of azides with alkynes. 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 μM. The obtained compounds induce caspase-3 activation and DNA fragmentation prevalently in follicular human thyroid cancer cell lines. |
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| Keywords: | Modified nucleosides Click-chemistry Antitumor agents 1 3-Dipolar cycloaddition FTC-133 and 8305C cell lines |
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