Litcius/Paper detail

Synthesis and<i>in vitro</i>anticancer activities of selenium<i>N</i>‐heterocyclic carbene compounds

Sheng Huang, Xinyu Sheng, Mianli Bian, Zhibin Yang, Yunlong Lu, Wukun Liu

2021Chemical Biology & Drug Design25 citationsDOI

Abstract

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.

Topics & Concepts

CytotoxicityCarbeneChemistryEbselenIn vitroReactive oxygen speciesApoptosisSeleniumCancer cellCell cultureStereochemistryBiochemistryCombinatorial chemistryBiologyCancerGlutathioneOrganic chemistryEnzymeCatalysisGeneticsGlutathione peroxidaseN-Heterocyclic Carbenes in Organic and Inorganic ChemistryGenomics, phytochemicals, and oxidative stressSynthesis and Biological Evaluation
Synthesis and<i>in vitro</i>anticancer activities of selenium<i>N</i>‐heterocyclic carbene compounds | Litcius