| Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores | |
Huang, Mingqin1; Duan, Shengzu1; Ma, Xueqiong1; Cai, Bicheng1,2; Wu, Dongmei1,2; Li, Yan2 ; Li, Liang1; Zhang, Hongbin1; Yang, Xiaodong1
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| 通讯作者 | Li, Yan(liyanb@mail.kib.ac.cn) ; Li, Liang(liliang5758@sina.com) ; Yang, Xiaodong(xdyang@ynu.edu.cn) |
| 2019-06-01 | |
| 发表期刊 | MEDCHEMCOMM
 |
| ISSN | 2040-2503 |
| 卷号 | 10期号:6页码:1027-1036 |
| 摘要 | The synthesis of a series of novel aza-brazilan derivatives containing imidazolium salt pharmacophores is presented. The biological activity of such imidazolium salts was further evaluated in vitro against a panel of human tumor cell lines. The results suggest that the electron-withdrawing group on the aza-brazilan moiety, substituted 5,6-dimethyl-benzimidazole ring and substitution of the imidazolyl-3-position with a 4-methylbenzyl group were essential for modulating the cytotoxic activity. Compounds 55 and 39, bearing a 4-methylbenzyl substituent at position-3 of 5,6-dimethyl-benzimidazole, were found to be the most potent compounds with IC50 values of 0.52-1.30 mu M and 0.56-1.51 mu M against four human tumor cell lines investigated. Particularly, compound 57 exhibited inhibitory activity against the MCF-7 cell line with an IC50 value of 0.35 mu M and was 56-fold more sensitive than DDP. Moreover, compound 55 inhibited cell proliferation through inducing G0/G1 cell cycle arrest and apoptosis in SMMC-7721 cells. |
| DOI | 10.1039/c9md00112c |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000472215900017 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/67184 |
| 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, Yan; Li, Liang; Yang, Xiaodong |
| 作者单位 | 1.Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resource, Minist Educ & Yunnan Prov, Kunming 650091, Yunnan, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Yunnan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Huang, Mingqin,Duan, Shengzu,Ma, Xueqiong,et al. Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores[J]. MEDCHEMCOMM,2019,10(6):1027-1036. |
| APA | Huang, Mingqin.,Duan, Shengzu.,Ma, Xueqiong.,Cai, Bicheng.,Wu, Dongmei.,...&Yang, Xiaodong.(2019).Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores.MEDCHEMCOMM,10(6),1027-1036. |
| MLA | Huang, Mingqin,et al."Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores".MEDCHEMCOMM 10.6(2019):1027-1036. |
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| huang2019.pdf（3833KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | 浏览 下载 | |
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