| Synthesis and antitumor activity of novel N-substituted carbazole imidazolium salt derivatives | |
Liu, Lan-Xiang; Wang, Xue-Quan; Zhou, Bei; Yang, Li-Juan; Li, Yan ; Zhang, Hong-Bin; Yang, Xiao-Dong
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| 2015-08-19 | |
| Source Publication | SCIENTIFIC REPORTS
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| Volume | 5 |
| Abstract | A series of novel N-substituted carbazole imidazolium salt derivatives has been prepared and investigated for their cytotoxic activity against five human tumor cell lines by MTS assay. The results indicated that the existence of 5,6-dimethyl-benzimidazole ring, substitution of the imidazolyl-3-position with a 2-bromobenzyl or naphthylacyl group, as well as alkyl chain length between carbazole and imidazole ring were important for the antitumor activity. Compound 61, bearing a 2-bromobenzyl substituent at position-3 of the 5,6-dimethyl-benzimidazole, showed powerful inhibitory activities and was more selective to HL-60, SMMC-7721, MCF-7 and SW480 cell lines with IC50 values 0.51-2.48 mu M. Mechanism of action studies revealed that this new compound could remarkably induce cell cycle arrest and apoptosis in SMMC-7721 cells. This work provides alternative novel way for future drug development based on carbazole and imidazolium salt scaffolds. |
| DOI | 10.1038/srep13101 |
| Indexed By | SCI |
| Language | 英语 |
| WOS ID | WOS:000359692000001 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.kib.ac.cn/handle/151853/25098 |
| Collection | 植物化学与西部植物资源持续利用国家重点实验室 |
| Recommended Citation GB/T 7714 | Liu, Lan-Xiang,Wang, Xue-Quan,Zhou, Bei,et al. Synthesis and antitumor activity of novel N-substituted carbazole imidazolium salt derivatives[J]. SCIENTIFIC REPORTS,2015,5. |
| APA | Liu, Lan-Xiang.,Wang, Xue-Quan.,Zhou, Bei.,Yang, Li-Juan.,Li, Yan.,...&Yang, Xiao-Dong.(2015).Synthesis and antitumor activity of novel N-substituted carbazole imidazolium salt derivatives.SCIENTIFIC REPORTS,5. |
| MLA | Liu, Lan-Xiang,et al."Synthesis and antitumor activity of novel N-substituted carbazole imidazolium salt derivatives".SCIENTIFIC REPORTS 5(2015). |
| Files in This Item: | Download All | |||||
| File Name/Size | DocType | Version | Access | License | ||
| srep13101.pdf（1438KB） | 期刊论文 | 作者接受稿 | 开放获取 | CC BY-NC-SA | View Download | |
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