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Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Arylaminoacetylhydrazone Derivatives Containing Carbazole Moiety

文献类型：期刊论文

作者Li Yingjun1; Lin Ledi1; Jin Kun2; Gao Lixin3; Sheng Li3; Liu Jihong4; Li Jia3
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
出版日期2021-08-25
卷号41期号:8页码:3157-3170
关键词protein tyrosine phosphatase 1B (PTP1B) inhibitor carbazole arylaminoacetylhydrazone synthesis molecular docking
ISSN号0253-2786
DOI10.6023/cjoc202102046
通讯作者Li Yingjun(chemlab.lnnu@163.com) ; Li Jia(jli@simm.ac.cn)
英文摘要In order to find novel protein tyrosine phosphatase 1B (PTP1B) inhibitors, a series of novel arylaminoacetylhydrazone derivatives containing carbazole moiety were designed and synthesized. Their structures and configurations were confirmed by IR, H-1 NMR, C-13 NMR, two-dimensional NMR spectra (including H-1-H-1 COSY, H-1-C-13 HMBC and NOESY) and elemental analysis. The inhibitory activities of all the target compounds against PTP1B were tested, and it was found that the target compounds had potent inhibitory activity against PTP1B, and most of them had lower IC50 value than the positive control drug oleanolic acid. Among them, N'-(9-octylcarbazol-3-ylmethylene)-2-(4-nitrophenylamino)acetohydrazide (3t) had the highest inhibitory activity against PTP1B with IC50 of (2.78 +/- 0.04) mu mol/L. Molecular docking was used to study the bind of compound 3t with PTP1B enzyme.
WOS关键词BREAST-CANCER CELLS ; MOLECULAR DOCKING ; ANTIVIRAL EVALUATION ; ACYLHYDRAZONE DERIVATIVES ; IN-SILICO ; PROMOTES ; DESIGN
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:000702991300019
出版者SCIENCE PRESS
源URL[http://119.78.100.183/handle/2S10ELR8/297578]  
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.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Liaoning, Peoples R China
2.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Liaoning, Peoples R China
3.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
4.Dalian Univ Technol, Chem Anal & Inspect Ctr, Dalian 116023, Liaoning, Peoples R China
推荐引用方式
GB/T 7714		 Li Yingjun,Lin Ledi,Jin Kun,et al. Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Arylaminoacetylhydrazone Derivatives Containing Carbazole Moiety[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2021,41(8):3157-3170.
APA Li Yingjun.,Lin Ledi.,Jin Kun.,Gao Lixin.,Sheng Li.,...&Li Jia.(2021).Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Arylaminoacetylhydrazone Derivatives Containing Carbazole Moiety.CHINESE JOURNAL OF ORGANIC CHEMISTRY,41(8),3157-3170.
MLA Li Yingjun,et al."Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Arylaminoacetylhydrazone Derivatives Containing Carbazole Moiety".CHINESE JOURNAL OF ORGANIC CHEMISTRY 41.8(2021):3157-3170.

入库方式： OAI收割

来源：上海药物研究所

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