synthesischaracterizationandbiologicalactivitiesof356trisubstituted124triazinederivatives
文献类型：期刊论文
| 作者 | Li YJ(李英俊)1; Shi XL(史相玲)1; Gao LX(高立信)2; Jin K(靳焜)3; Sheng L(盛丽)2; Wu JH(吴疆红)1; Peng LN(彭立娜)1; Li J(李佳)2
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| 刊名 | chinesejournaloforganicchemistry
 |
| 出版日期 | 2015 |
| 卷号 | 35期号:1页码:191 |
| 关键词 | MICROWAVE-ASSISTED SYNTHESIS BENZIMIDAZOLE DERIVATIVES ANTITUMOR-ACTIVITY COMPLEXES CYTOTOXICITY DESIGN 3,5,6-trisubstituted-1,2,4-triazine benzimidazole microwave irradiation synthesis crystal structure Cdc25B and PTP1B inhibitors |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201405032 |
| 英文摘要 | Thirty new 3,5,6-trisubstituted-1,2,4-triazine derivatives containing benzimidazole moiety (5 similar to 6) were synthesized via microwave-assisted condensation reactions of 2-aryloxymethylbenzimidazole-1-acetylhydrazines (3) with benzil/p-anisil in the presence of NH4OAc/HOAc. The structures were characterized by elemental analysis, IR, H-1 NMR spectra and single crystal X-ray determination. The synthesized target compounds were evaluated for Cdc25B and PTP1B inhibitory activities. The structure-activity relationship (SAR) was also briefly discussed. The experimental results indicated that some compounds showed good inhibitory activities against Cdc25B and PTP1B. Among of them, compound 6o IC50 =(0.84 +/- 0.22) mu g/mL. exhibited highest inhibitory activity against Cdc25B. Compounds 5i, 5m, 5n, 6h, 6j, 6m, 6n and 6o showed higher inhibitory activities against PTP1B IC50=(0.46 +/- 0.10)similar to(0.87 +/- 0.19) mu g/mL than positive control oleanolic acid IC50=(0.97 +/- 0.15) mu g/mL. It is noteworthy that, compounds 5h, 5m, 6n and 6o showed inhibitory activities against Cdc25B and PTP1B. The target compounds can be considered as potential Cdc25B and PTP1B inhibitors. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/286104]  |
| 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 | Li YJ,Shi XL,Gao LX,et al. synthesischaracterizationandbiologicalactivitiesof356trisubstituted124triazinederivatives[J]. chinesejournaloforganicchemistry,2015,35(1):191. |
| APA | 李英俊.,史相玲.,高立信.,靳焜.,盛丽.,...&李佳.(2015).synthesischaracterizationandbiologicalactivitiesof356trisubstituted124triazinederivatives.chinesejournaloforganicchemistry,35(1),191. |
| MLA | 李英俊,et al."synthesischaracterizationandbiologicalactivitiesof356trisubstituted124triazinederivatives".chinesejournaloforganicchemistry 35.1(2015):191. |
入库方式： OAI收割
来源：上海药物研究所
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