Synthesis and anticancer activity of a hydroxytolan series

This paper describes the development of novel anticancer poly-hydroxylated tolans. Based on structural similarity to resveratrol, a series of hydroxytolans were synthesized and evaluated for their antitumor capability against three tumor cell lines and one fibroblast cell line for selectivity comparisons. The 4,4′-dihydroxytolan (KST-201) exhibited the most significant anticancer activity with increased selectivity when compared to resveratrol and other hydroxytolans. Unlike resveratrol, KST-201 can boost hydrogen peroxide in tumor cells, which are often at high basal level of reactive oxygen species, to cause cell death by overwhelming the cellular tolerance of oxidative stress.

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