Abstract

Chalcones are a wide-range of natural and synthetic compounds with several pharmacological applications, highlighting their antiproliferative action on multiple cancer cell lines. In this study, their synthesis and preliminary evaluation as cytotoxic agent on breast cancer (MCF-7) and colorectal cancer (Caco-2) cell lines, as well as, their evaluation on non-cancer human fibroblast is shown. The synthesis showed high yields (55% a 99%), while cytotoxic assays showed high activity and selectivity on MCF-7, mainly for chalcones with a 3’,4’-(OCH2O) substitution pattern (compound 5g IC50= 2.3µM; SI= 9.1). In the case of Caco-2, the best result were obtained with chalcones with a 3’-OMe substitution pattern (compound 5c IC50= 18.0µM; SI= 2.0). This evaluation, although preliminary, suggests that the substitution pattern 3',4' - (OCH2O) for MCF-7 and the 3'-OMe substitution for Caco-2 are the avenue to follow for new antiproliferative agents development