In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole

Abstract

The investment in cancer research is critical to find more and better treatments, but essentially to save lives. Here, we describe the synthesis and characterization on new bromothiazole derivatives with amino acids and with core of nitazoxanide, an FDA-approved antiprotozoal drug. Using a human adenocarcinoma-derived cell line (the Caco-2 cell line), we then investigated the antiproliferative (³H-thymidine incorporation) and cytotoxic (extracellular lactate dehydrogenase activity) effect of these derivatives. All the derivatives caused a concentration-dependent decrease in cell proliferation and viability. At their highest concentration, all compounds were able to reduce ³H-thymidine incorporation by more than 80%, corresponding to a more marked antiproliferative effect than butyrate. As to their cytotoxic effect, it was comparable to that of butyrate. The ability of bromo substituent in thiazole ring with new sequences of amino acids in inducing cell death and apoptosis in Caco-2 cells (and other cell lines) is now being studied.

Keywords: (3)H-thymidine incorporation; Bromothiazole; Caco-2 cell; Colorectal cancer; Extracellular dehydrogenase activity.