Abstract: The synthesis in water of new sulfone derivatives under microwave irradiation is described. This eco-friendly process leads to the expected products in good yields by reaction of various substituted sulfinates (commercially available or obtained by reduction of the corresponding sulfonyl chlorides) with 4-chloromethyl-2-methyl-5-nitro-1,3-thiazole. In order to evaluate the antiproliferative effect of these compounds, several sulfone derivatives are also dichlorinated on the Cα next to the sulfonyl group. An evaluation on different cancer cell lines reveals promising selective in vitro antiproliferative activity toward HepG2 human cell lines by dihydrogenated sulfones, suggesting further research should be to explore their anticancer potential in the treatment of liver cancer.
Keywords: 5-nitrothiazole; sulfones; microwave irradiation; in vitro antiproliferative; HepG2 cell line; activity cellular specificity
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Cohen, A.; Crozet, M.D.; Rathelot, P.; Azas, N.; Vanelle, P. Synthesis and Promising in Vitro Antiproliferative Activity of Sulfones of a 5-Nitrothiazole Series. Molecules 2013, 18, 97-113.
Cohen A, Crozet MD, Rathelot P, Azas N, Vanelle P. Synthesis and Promising in Vitro Antiproliferative Activity of Sulfones of a 5-Nitrothiazole Series. Molecules. 2013; 18(1):97-113.
Cohen, Anita; Crozet, Maxime D.; Rathelot, Pascal; Azas, Nadine; Vanelle, Patrice. 2013. "Synthesis and Promising in Vitro Antiproliferative Activity of Sulfones of a 5-Nitrothiazole Series." Molecules 18, no. 1: 97-113.