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Updated: Jan 16, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and antitumor activity of steroid-based imidazolium salts
Tingting Li1, Yu Pan1, Yuanyuan Peng1
1Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Key Laboratory of Research and Development for Natural Products, School of Pharmacy, Yunnan University Kunming 650500 P. R. China konglingmei@ynu.edu.cn ggdeng@ynu.edu.cn.
Abstract:
A total of thirty-six novel diosgenin-, cholesterol-, and dehydroepiandrosterone-imidazolium salt derivatives were synthesized and their cytotoxic activities were evaluated in vitro against a panel of human tumor cell lines. The SAR results indicated that the presence of a substituted 5,6-dimethylbenzimidazole ring and the substitution at the imidazolyl-3-position with a 1-naphthylmethyl or 4-methylbenzyl group could be critical for enhancing cytotoxic activity. Dehydroepiandrosterone-imidazolium salt 12f was found to be the most potent compound with IC50 values of 1.07-2.10 μM against MDA-MB-231, HepG2 and 22RV1 human tumor cell lines. Furthermore, cell cycle and apoptosis experiments of compound 12f were carried out and the results showed that 12f could induce G0/G1 cell cycle arrest and apoptosis in HepG2-116 cells.
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