| Synthesis and cytotoxic activity of novel 1-((indol-3-yl)methyl)-1H-imidazolium salts | |
Xu, Xiao-Liang1; Wang, Jia1; Yu, Chun-Lei2; Chen, Wen1; Li, Ying-Chao1; Li, Yan2 ; Zhang, Hong-Bin1; Yang, Xiao-Dong1; Li,Y (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650204,Peoples R China.; liyanb@mail.kib.ac.cn; zhanghbyd@gmail.com; xdyang@ynu.edu.cn
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| 2014-11-01 | |
| 发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| ISSN | 0960-894X |
| 卷号 | 24期号:21页码:4926-4930 |
| 摘要 | A series of novel 1-((indol-3-yl) methyl)-1H-imidazolium salts were prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 5,6-dimethyl-benzimidazole ring, and substitution of the imidazolyl-3-position with a naphthylacyl or 4-bromophenacyl group, were vital for modulating inhibitory activity of cell growth. In particular, 1-((N-Boc-indol-3-yl)methyl)-3-(2-naphthylacyl)-1H-5,6-dimethyl-benzimidazolium bromide was found to be the most potent derivative and more selective against myeloid liver carcinoma (SMMC-7721), lung carcinoma (A549) and breast carcinoma (MCF-7), with IC50 values 1.9-fold, 1.7-fold and 4.8-fold lower than DDP. This compound can induce significant cell apoptosis in SMMC-7721 cells. (C) 2014 Elsevier Ltd. All rights reserved. NH |
| 关键词 | Indole Imidazolium Salts Structure-activity Relationships Cell Apoptosis |
| 学科领域 | Pharmacology & Pharmacy ; Chemistry |
| DOI | 10.1016/j.bmcl.2014.09.045 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS记录号 | WOS:000343309800002 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/18379 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 通讯作者 | Li,Y (reprint author),Chinese Acad Sci,Kunming Inst Bot,State Key Lab Phytochem & Plant Resources West Ch,Kunming 650204,Peoples R China.; liyanb@mail.kib.ac.cn; zhanghbyd@gmail.com; xdyang@ynu.edu.cn |
| 作者单位 | 1.Yunnan Univ, Sch Chem Sci & Technol, Minist Educ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xu, Xiao-Liang,Wang, Jia,Yu, Chun-Lei,et al. Synthesis and cytotoxic activity of novel 1-((indol-3-yl)methyl)-1H-imidazolium salts[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(21):4926-4930. |
| APA | Xu, Xiao-Liang.,Wang, Jia.,Yu, Chun-Lei.,Chen, Wen.,Li, Ying-Chao.,...&xdyang@ynu.edu.cn.(2014).Synthesis and cytotoxic activity of novel 1-((indol-3-yl)methyl)-1H-imidazolium salts.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24(21),4926-4930. |
| MLA | Xu, Xiao-Liang,et al."Synthesis and cytotoxic activity of novel 1-((indol-3-yl)methyl)-1H-imidazolium salts".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24.21(2014):4926-4930. |
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