36二取代124三嗪衍生物的微波辅助合成及生物活性
文献类型：期刊论文
| 作者 | 李英俊1; 邵昕1; 高立新2; 靳焜3; 盛丽2; 罗潼川1; 于洋1; 李佳2
|
| 刊名 | 有机化学
 |
| 出版日期 | 2013 |
| 卷号 | 33期号:10页码:2178 |
| 关键词 | ONE-POT SYNTHESIS BENZIMIDAZOLE DERIVATIVES 1,2,4-TRIAZINES AGENTS INHIBITORS PTP1B microwave irradiation 1,2,4-triazines benzimidazole synthesis Cdc25B and PTP1B inhibitors |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201304011 |
| 英文摘要 | Twenty new 3,6-disubstituted-1,2,4-triazine derivatives containing benzimidazole moiety (4) were synthesized via microwave-assisted condensation reactions of 2-aryloxymethylbenzimidazole-1-acetylhydrazines (3) with various (un)substituted phenacyl bromides in DMF. The structures were characterized by IR, H-1 NMR spectra and elemental analysis. The optimum experimental conditions were found. Compared with traditional methods, this synthetic method has such advantages as short reaction time, simple operation, broad substrate scope, easy purification and high yields. The synthesized target compounds were screened for Cdc25B and PTP1B inhibitory activities. The experimental results indicate that compounds 4g and 4j showed good inhibitory activities against Cdc25B, and 4a, 4h, 4j, 4r and 4s exhibited potent inhibitory activities against PTP1B. It is noteworthy that compound 4j can be used as potential Cdc25B and PTP1B inhibitors in the treatment of cancer and diabetes. |
| 资助项目 | [Natural Science Foundation of Liaoning Province] |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/288353]  |
| 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.中国科学院上海药物研究所 3.大连理工大学 |
| 推荐引用方式 GB/T 7714 | 李英俊,邵昕,高立新,等. 36二取代124三嗪衍生物的微波辅助合成及生物活性[J]. 有机化学,2013,33(10):2178. |
| APA | 李英俊.,邵昕.,高立新.,靳焜.,盛丽.,...&李佳.(2013).36二取代124三嗪衍生物的微波辅助合成及生物活性.有机化学,33(10),2178. |
| MLA | 李英俊,et al."36二取代124三嗪衍生物的微波辅助合成及生物活性".有机化学 33.10(2013):2178. |
入库方式： OAI收割
来源：上海药物研究所
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