Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity
文献类型：期刊论文
| 作者 | Li Yingjun2; Wang Siyuan2; Jin Kun3; Gao Lixin1; Sheng Li1; Zhang Nan2; Liu Jihong4; Li Jia1
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2019-02-25 |
| 卷号 | 39期号:2页码:491-499 |
| 关键词 | acylhydrazone carbazole synthesis Cdc25B and PTP1B inhibitor molecular docking |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201806042 |
| 通讯作者 | Li Yingjun(chemlab.lnnu@163.com) ; Li Jia() |
| 英文摘要 | A series of novel acylhydmzone derivatives 6 containing carbazole moity were synthesized by carbazole and 4-cyanobenzyl chloride as starting materials via multi-step reactions. Their structures were characterized by IR, H-1 NMR, C-13 NMR spectra and elemental analysis. All synthesized target compounds were evaluated for the inhibitory activities against Cdc25B and PTP1B. The results show that the target compounds display significant inhibitory activities against Cdc25B/PTP1B. Among them, compound 4-((carbazol-9-yl)methyl),N'-(2-hydroxy-1-naphthaleny hnethylene)benzoyl hydrazide (6g) had the highest inhibitory activities against Cdc25B and PTP1B with IC50 values of (2.16 +/- 0.38) and (1.06 +/- 0.23) mu g/mL, respectively. The molecular docking results indicated that the hydrogen bond and hydrophobic interaction formed between compound 6g and Cdc25B/PTP1B enzyme. |
| WOS关键词 | BIOLOGICAL EVALUATION ; ANTITUBERCULOSIS ACTIVITY ; PHOSPHATASE INHIBITORS ; ANTIMICROBIAL ACTIVITY ; DOCKING ; OPTIMIZATION ; MECHANISM ; ANALOGS ; DESIGN ; AGENTS |
| 资助项目 | Natural Science Foundation of Liaoning Province[20102126] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000458607700023 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/290485]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Li Yingjun; Li Jia |
| 作者单位 | 1.Chinese Acad Sci, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China 3.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China 4.Dalian Univ Technol, Chem Anal & Res Ctr, Fac Chem Environm & Biol Sci & Technol, Dalian 116023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li Yingjun,Wang Siyuan,Jin Kun,et al. Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2019,39(2):491-499. |
| APA | Li Yingjun.,Wang Siyuan.,Jin Kun.,Gao Lixin.,Sheng Li.,...&Li Jia.(2019).Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity.CHINESE JOURNAL OF ORGANIC CHEMISTRY,39(2),491-499. |
| MLA | Li Yingjun,et al."Synthesis and Cdc25B/PTP1B Inhibitory Activity Evaluation of Novel Acylhydrazone Derivatives Containing Carbazole Moity".CHINESE JOURNAL OF ORGANIC CHEMISTRY 39.2(2019):491-499. |
入库方式： OAI收割
来源：上海药物研究所
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