One-pot synthesis and evaluation of novel 3-aryl-6-ethoxycarbonyl-4-hydroxy-2H-pyran-2-one as a potent cytotoxic agent

Abstract

A series of new open chain analogs of Phelligridin J were synthesized by a clean one-pot approach. These compounds were evaluated for their in vitro cytotoxicity against normal and breast cancer cell lines. All the compounds exhibited potent cytotoxic activity in the lower micro molar range. Compound 5o exhibited the maximum cytotoxic activity with IC₅₀ values of 12.49 and 13.76 μM, whereas compound 5a showed two-fold selectivity viz. IC₅₀ values of 21.80 to 43.40 μM against breast cancer (MCF7) and normal fibroblast (NIH3T3) cell lines, respectively.