1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors

doi:10.3390/molecules19010102

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	1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
	Wang, Wen-Long 1,2,3; Yang, Dong-Lin 2; Gao, Li-Xin 1; Tang, Chun-Lan 1; Ma, Wei-Ping 1; Ye, Hui-Hua 2; Zhang, Si-Qi 2; Zhao, Ya-Nan 2; Xu, Hao-Jie 2; Hu, Zhao 2
刊名	MOLECULES
	2014-01
卷号	19 期号:1 页码:102-121
关键词	1H-2,3-dihydroperimidine derivatives PTP1B inhibitors selectivity structure-activity relationships (SAR)
ISSN号	1420-3049
DOI	10.3390/molecules19010102
文献子类	Article
英文摘要	A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
资助项目	National Natural Science Foundation of China[81125023] ; State Key Laboratory of Drug Research[SIMM1302KF-05] ; Fundamental Research Funds for the Central Universities[JUSRP1040]
WOS关键词	MOLECULE KINASE INHIBITORS ; INSULIN SENSITIVITY ; DRUG TARGETS ; CANCER ; PTP1B ; MICE ; DISCOVERY ; MECHANISM
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	MDPI AG
WOS记录号	WOS:000334420300007
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277293]
专题	国家新药筛选中心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	Wang, Wen-Long
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Peoples R China; 3.Jiangshu Alpha Biopharmaceut Inc, Wuxi 214122, Peoples R China
推荐引用方式 GB/T 7714	Wang, Wen-Long,Yang, Dong-Lin,Gao, Li-Xin,et al. 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors[J]. MOLECULES,2014,19(1):102-121.
APA	Wang, Wen-Long.,Yang, Dong-Lin.,Gao, Li-Xin.,Tang, Chun-Lan.,Ma, Wei-Ping.,...&Feng, Bainian.(2014).1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors.MOLECULES,19(1),102-121.
MLA	Wang, Wen-Long,et al."1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors".MOLECULES 19.1(2014):102-121.