Synthesis and Cell Division Cycle 25B Phosphatase/Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel Acylthiourea Derivatives
文献类型：期刊论文
| 作者 | Li Yingjun2; Wang Siyuan2; Jin Kun1; Gao Lixin3; Sheng Li3; Zhang Nan2; Yang Kaidong2; Zhao Yue2; Li Jian3 |
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2018-05-25 |
| 卷号 | 38期号:5页码:1242-1250 |
| 关键词 | acylthiourea carbazole synthesis Cdc25B and PTP1B inhibitors molecular docking |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201709022 |
| 文献子类 | Article |
| 英文摘要 | A series of new acylthiourea derivatives 3 containing carbazole moity have been synthesized by the techniques of ultrasonic irradiation and solid-liquid phase transfer catalysis. Their structures were characterized by IR, H-1 NMR, C-13 NMR spectra and elemental analysis. This synthetic method has the advantages of short reaction time, simple operation and high yield. All synthesized target compounds were screened for their inhibitory activity against cell division cycle 25B phosphatase (Cdc25B) and protein tyrosine phosphatase 1B (PTP1B). The results show that all the compounds 3 display significant inhibitory activities against Cdc25B, and partial target compounds 3 also show significant inhibitory activities against PTP1B. Among them, 1-(4-nitrobenzoy1)-3-(9-ethyl-carbazole-3-yl)thiourea (3n) exhibits highest inhibitory activity against Cdc25B [IC50 = (0.49 +/- 0.12) mu g/mL] and 1-(2-nitrobenzoy1)-3-(9-ethyl-carbazole-3-yl)thiourea (31) displays highest inhibitory activity against PTP1B [IC50 =(3.59 +/- 1.15) mu g/mL]. It is noteworthy that compound 3n shows higher inhibitory activity against Cdc25B and PTP1B. The preliminary research results of molecular docking revealed the structural-activity of the inhibitors. The active compounds can be considered as potential Cdc25B and PTP1B inhibitors, and have great application prospects in the treatment of cancers and diabetes. |
| WOS关键词 | BIOLOGICAL EVALUATION ; IN-VITRO ; CARBAZOLE ALKALOIDS ; ANTIBACTERIAL ACTIVITIES ; PTP1B INHIBITORS ; ACID-DERIVATIVES ; ANTITUMOR AGENT ; ACYL-THIOUREA ; IDENTIFICATION ; ANALOGS |
| 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:6237587 |
| WOS记录号 | WOS:000440483900025 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279740]  |
| 专题 | 药物化学研究室 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 |
| 通讯作者 | Li Yingjun; Li Jian |
| 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,Wang Siyuan,Jin Kun,et al. Synthesis and Cell Division Cycle 25B Phosphatase/Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel Acylthiourea Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2018,38(5):1242-1250. |
| APA | Li Yingjun.,Wang Siyuan.,Jin Kun.,Gao Lixin.,Sheng Li.,...&Li Jian.(2018).Synthesis and Cell Division Cycle 25B Phosphatase/Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel Acylthiourea Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,38(5),1242-1250. |
| MLA | Li Yingjun,et al."Synthesis and Cell Division Cycle 25B Phosphatase/Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel Acylthiourea Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 38.5(2018):1242-1250. |
入库方式： OAI收割
来源：上海药物研究所
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