Synthesis and cytotoxic activity of novel 1-((indol-3-yl)methyl)-1H-imidazolium salts
文献类型:期刊论文
作者 | Xu, Xiao-Liang1; Wang, Jia1; Yu, Chun-Lei2; Chen, Wen1; Li, Ying-Chao1; Li, Yan2![]() |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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出版日期 | 2014-11-01 |
卷号 | 24期号:21页码:4926-4930 |
关键词 | Indole Imidazolium salts Structure-activity relationships Cell apoptosis |
ISSN号 | 0960-894X |
产权排序 | 第二 |
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 |
英文摘要 | 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 |
学科主题 | Pharmacology & Pharmacy ; Chemistry |
类目[WOS] | Chemistry, Medicinal ; Chemistry, Organic |
研究领域[WOS] | Pharmacology & Pharmacy ; Chemistry |
关键词[WOS] | ANTITUMOR-ACTIVITY ; MARINE SPONGE ; DESIGN ; DERIVATIVES ; PRODUCTS ; IODIDES ; ANALOGS ; TRANS |
收录类别 | SCI ; IC |
资助信息 | Program for Changjiang Scholars and Innovative Research Team in University [IRT13095]; Natural Science Foundation of China [21462049, 21332007]; Yunnan Province [2013FA028, 2012FB113, 2010GA014]; Project of Recruited Top Talent of Sciences and Technology of Yunnan Province [2009C1120]; 100 Talents Program of Chinese Academy of Science |
语种 | 英语 |
WOS记录号 | WOS:000343309800002 |
公开日期 | 2014-11-25 |
源URL | [http://ir.kib.ac.cn/handle/151853/18379] ![]() |
专题 | 昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室 |
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.,...&Yang, Xiao-Dong.(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. |
入库方式: OAI收割
来源:昆明植物研究所
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