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Synthesis and biological evaluation of 3-hydroxymethyl-5-(1H-1,2,3-triazol) isoxazolidines

2013; Elsevier BV; Volume: 21; Issue: 24 Linguagem: Inglês

10.1016/j.bmc.2013.10.001

1464-3391

Roberto Romeo, Salvatore V. Giofrè, Caterina Carnovale, Agata Campisi, Rosalba Parenti, Lorenzo Bandini, Maria Assunta Chiacchio,

Chemical Synthesis and Analysis

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.