新型咪唑21b134噻二唑衍生物的合成及cdc25b抑制活性
文献类型：期刊论文
| 作者 | 李英俊1; 罗潼川1; 靳焜2; 高立信3; 邵昕1; 盛丽3; 于洋1; 李佳3
|
| 刊名 | 有机化学
 |
| 出版日期 | 2014 |
| 卷号 | 34期号:2页码:325 |
| 关键词 | BIOLOGICAL-ACTIVITIES AGENTS MOIETY ACID imidazo2,1-b1,3,4thiadiazole microwave-assisted synthesis Cdc25B |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201309013 |
| 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-imidazo2,1-b1,3,4thiadiazoles 4 have been synthesized by microwave-assisted method. Then nineteen novel 2,6-diaryl-imidazo2,1-b1,3,4thiadiazole-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. |
| 资助项目 | [Natural Science Foundation of Liaoning Province] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/284715]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.辽宁师范大学 2.大连理工大学 3.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | 李英俊,罗潼川,靳焜,等. 新型咪唑21b134噻二唑衍生物的合成及cdc25b抑制活性[J]. 有机化学,2014,34(2):325. |
| APA | 李英俊.,罗潼川.,靳焜.,高立信.,邵昕.,...&李佳.(2014).新型咪唑21b134噻二唑衍生物的合成及cdc25b抑制活性.有机化学,34(2),325. |
| MLA | 李英俊,et al."新型咪唑21b134噻二唑衍生物的合成及cdc25b抑制活性".有机化学 34.2(2014):325. |
入库方式： OAI收割
来源：上海药物研究所
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