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

doi:10.6023/cjoc202102046

	Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Arylaminoacetylhydrazone Derivatives Containing Carbazole Moiety
	Li Yingjun 1; Lin Ledi 1; Jin Kun 2; Gao Lixin 3; Sheng Li 3; Liu Jihong 4; Li Jia 3
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	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
DOI	10.6023/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.
资助项目	Natural Science Foundation of Liaoning Province[20102126]
WOS关键词	BREAST-CANCER CELLS ; MOLECULAR DOCKING ; ANTIVIRAL EVALUATION ; ACYLHYDRAZONE DERIVATIVES ; IN-SILICO ; PROMOTES ; DESIGN
WOS研究方向	Chemistry
语种	英语
出版者	SCIENCE PRESS
WOS记录号	WOS:000702991300019
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297578]
专题	中国科学院上海药物研究所
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.