Synthesis and Cytotoxic Activity of Novel Ergosterol Peroxide Derivatives with Acrylate or Propionate Side Chain

A series of novel ergosterol peroxide derivatives with acrylate or propionate side chain were synthesized. All compounds 3a-n were evaluated for their cytotoxicity against four kinds of human carcinoma cell lines (HepG2, MCF-7, HCT-116, and A549). Most of the derivatives displayed stronger cytotoxicity than ergosterol peroxide parent. Among them, compound 3h with the highest potency against HepG2 cell line (IC50  =  2.70 μM), which was 7.47-fold more efficacious than ergosterol peroxide. The results suggested that the introduction of acrylate or propionate side chain at C-3 position of ergosterol peroxide is beneficial to enhance its cytotoxic activity. Compound 3h has potential to become a novel anti-tumor agent through further structural modification.