Synthesis and Cdc25B Inhibition Activity of Novel Imidazo[2,1-b][1,3,4]thiadiazole Derivatives
文献类型：期刊论文
| 作者 | Li Yingjun2; Luo Tongchuan2; Jin Kun1; Gao Lixin3; Shao Xin2; Sheng Li3; Yu Yang2; Li Jia3
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2014-02 |
| 卷号 | 34期号:2页码:325-333 |
| 关键词 | imidazo[2,1-b][1,3,4]thiadiazole microwave-assisted synthesis Cdc25B |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201309013 |
| 文献子类 | Article |
| 英文摘要 | Researches indicate that the cell division cycle 25 phosphatase B (Cdc25B) is over-expressed in various primary human cancers-including breast, colon, cervix, lung, etc. This suggests that the inhibition of Cdc25B may become a promising strategy in oncology. In this work, twenty novel 2,6-diaryl-imidazo[2,1-b][1,3,4]thiadiazoles 4 have been synthesized by microwave-assisted method. Then nineteen novel 2,6-diaryl-imidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehydes (5) have obtained by Vilsmeier-Haack reaction. The structures of new compounds 3, 4 and 5 were characterized by IR, H-1 NMR spectra and elemental analysis. The synthesized target compounds 4 and 5 were screened for Cdc25B inhibitory activities. The results revealed that compound 4c showed the highest inhibitory activity against Cdc25B With percentage inhibition 87.68% at 5 mu g/mL, compounds 4o and Sc showed moderate activities with percentage inhibition 55.76% and 57.69%, respectively. They can be considered as potential candidates as novel Cdc25B inhibitors. |
| WOS关键词 | BIOLOGICAL-ACTIVITIES ; AGENTS ; MOIETY ; ACID |
| 资助项目 | Natural Science Foundation of Liaoning Province[20102126] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5079664 |
| WOS记录号 | WOS:000333499500007 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277196]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Li Yingjun |
| 作者单位 | 1.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China; 2.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li Yingjun,Luo Tongchuan,Jin Kun,et al. Synthesis and Cdc25B Inhibition Activity of Novel Imidazo[2,1-b][1,3,4]thiadiazole Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2014,34(2):325-333. |
| APA | Li Yingjun.,Luo Tongchuan.,Jin Kun.,Gao Lixin.,Shao Xin.,...&Li Jia.(2014).Synthesis and Cdc25B Inhibition Activity of Novel Imidazo[2,1-b][1,3,4]thiadiazole Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,34(2),325-333. |
| MLA | Li Yingjun,et al."Synthesis and Cdc25B Inhibition Activity of Novel Imidazo[2,1-b][1,3,4]thiadiazole Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 34.2(2014):325-333. |
入库方式： OAI收割
来源：上海药物研究所
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