A synthetic approach towards a series of3-hydroxymethyl-5-(1H-1,2,3-triazol)isoxazolidines has been reported, accordingto 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 inhibitproliferation of follicular and anaplastic human thyroid cancer cell lines, with IC50 values ranging from 3.87 to 8.76 lM. The obtained compounds induce caspase-3activation and DNA fragmentation prevalently in follicular human thyroid cancercell lines.
Synthesis and biological evaluation of 3-Hydroxymethyl-5-(1H-1,2,3-Triazol)-Isoxazolidines
CAMPISI, Agatina;PARENTI, Rosalba;CHIACCHIO, MARIA ASSUNTA ROSSELLA
2013-01-01
Abstract
A synthetic approach towards a series of3-hydroxymethyl-5-(1H-1,2,3-triazol)isoxazolidines has been reported, accordingto 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 inhibitproliferation of follicular and anaplastic human thyroid cancer cell lines, with IC50 values ranging from 3.87 to 8.76 lM. The obtained compounds induce caspase-3activation and DNA fragmentation prevalently in follicular human thyroid cancercell lines.File in questo prodotto:
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