Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors

doi:10.1016/j.ejmech.2011.05.027

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	Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors
	Sun, Liang-Peng 1; Shen, Qiang 2; Piao, Hong-Hua 1; Ma, Wei-Ping 2; Gao, Li-Xin 2; Zhang, Wei 2; Nan, Fa-Jun2 ; Li, Jia2 ; Piao, Hu-Ri 1
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2011-09
卷号	46 期号:9 页码:3630-3638
关键词	Protein tyrosine phosphatase 1B Inhibitors 2-Naphthol tyrosine SAR Diabetes
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2011.05.027
文献子类	Article
英文摘要	A series of novel nonphosphonate-based pTyr mimetics comprised (+/-)-3-(2-(2-fluorobenzyloxy)naphthalen-6-yl)-2-aminopropanoic acid derivatives were identified as reversible and competitive PTP1B inhibitors via a structure-based design approach. Among the compounds studied, 12h was found to have the best in vitro inhibition activity against PTP1B (IC(50) = 1.25 +/- 0.24 mu M) and the best selectivity (3-fold) between PTP1B and TCPTP. These results should provide suitable druglike lead compounds for the design of inhibitors of PTP1B as well as other PTPs. (C) 2011 Elsevier Masson SAS. All rights reserved.
资助项目	National Natural Science Foundation of China[20962021] ; National Science & Technology Major Project of China "Key New Drug Creation and Manufacturing Program"[2009ZX09302-001] ; National Science & Technology Major Project[2007CB914201] ; Natural Science Foundation of China[81021062] ; Natural Science Foundation of China[30801405] ; Shanghai Commission of Science and Technology[09DZ2291200]
WOS关键词	TYROSINE-PHOSPHATASE 1B ; INSULIN SIGNAL-TRANSDUCTION ; PROTEIN ; DISCOVERY ; OBESITY ; MICE ; SENSITIVITY ; SPECIFICITY ; RESISTANCE ; ADIPOSITY
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000295237400010
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278415]
专题	国家新药筛选中心药物发现与设计中心药物安全性评价中心
通讯作者	Piao, Hu-Ri
作者单位	1.Yanbian Univ, Key Lab Nat Resources Changbai Mt & Funct Mol, Minist Educ, Coll Pharm, Yanji 133000, Peoples R China; 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Sun, Liang-Peng,Shen, Qiang,Piao, Hong-Hua,et al. Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2011,46(9):3630-3638.
APA	Sun, Liang-Peng.,Shen, Qiang.,Piao, Hong-Hua.,Ma, Wei-Ping.,Gao, Li-Xin.,...&Piao, Hu-Ri.(2011).Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,46(9),3630-3638.
MLA	Sun, Liang-Peng,et al."Synthesis and biological evaluation of (+/-)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46.9(2011):3630-3638.