LIGIA BALANEAN, CORNELIA BRAICU, IOANA BERINDAN-NEAGOE, CRISTINA NASTASA, BRINDUSA TIPERCIUC, PHILIPPE VERITE, OVIDIU ONIGA<br>Synthesis of Novel 2-metylamino-4-substituted-1,3-thiazoles <br>with Antiproliferative Activity

LIGIA BALANEAN, CORNELIA BRAICU, IOANA BERINDAN-NEAGOE, CRISTINA NASTASA, BRINDUSA TIPERCIUC, PHILIPPE VERITE, OVIDIU ONIGA
Synthesis of Novel 2-metylamino-4-substituted-1,3-thiazoles
with Antiproliferative Activity

Abstract:

In the context of the continuous and increased interest in new biologically active thiazole analogues in medicinal chemistry, we proposed a research project that involves the synthesis of several agents bearing a 2-amino-thiazole core fused with thiophene or substituted 3-formylchromone and the investigation of their antiproliferative potential. Thus, a few new N’-2-(2-methylamino)thiazol-4-yl)acetohydrazide-hydrazones have been synthesized through the condensation of a hydrazide fragment with thiophene or different substituted 3-formylchromones. The structures of the newly obtained compounds have been confirmed by the combined use of elemental analysis and spectroscopic data (MS, 1H NMR and 13C NMR). The new molecules have undergone antiproliferative evaluation using MTT assay in three in vitro models, namely Hs578T, HeLa and Hep2G. The condensation of the thiazolic hydrazide-hydrazones with a chromone moiety has proven to be effective in respect to the antiproliferative activity, especially in the case of compound 3b, which showed excellent results on all three cancer cell lines used. Keywords: 2-Methyl-aminothiazole; Hydrazid-hydrazone; Antitumoral; 3-Formylchromones

Issue: 2014, Volume 65, Issue 12

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