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Synthesis and in vitro anticancer activities of selenium N ‐heterocyclic carbene compounds
Author(s) -
Huang Sheng,
Sheng Xinyu,
Bian Mianli,
Yang Zhibin,
Lu Yunlong,
Liu Wukun
Publication year - 2021
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13900
Subject(s) - cytotoxicity , carbene , chemistry , ebselen , in vitro , reactive oxygen species , apoptosis , selenium , cancer cell , cell culture , stereochemistry , biochemistry , combinatorial chemistry , biology , cancer , glutathione , organic chemistry , enzyme , genetics , catalysis , glutathione peroxidase
Fourteen novel selenium N ‐heterocyclic carbene (Se‐NHC) compounds derived from 4,5‐diarylimidazole were designed, synthesized, and evaluated as antiproliferative agents. Most of them were more effective toward A2780 ovarian cancer cells than HepG2 hepatocellular carcinoma cells. Among them, the most active compound 2b was about fourfold more active than the positive control ebselen against A2780 cells. In addition, this compound displayed twofold higher cytotoxicity to A2780 cells than to IOSE80 normal ovarian epithelial cells. Further studies revealed that 2b could induce reactive oxygen species production, damage mitochondrial membrane potential, block the cells in the G0/G1 phase, and finally promote A2780 cell apoptosis.