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Updated: Mar 16, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and anticancer activity of a hydroxytolan series
Boren Lin1, Karen McGuire1, Bo Liu1
1Department of Chemistry and Biochemistry, Kent State University, PO Box 5190, Kent, OH 44242-0001, United States.
Abstract:
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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