Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2

doi:10.6023/cjoc201603045

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	Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2
	Wang Wenlong 1; Luo Huan 1; Gao Ya 1; Gao Lixin 2; Sheng Li 2; Zhou Yubo2 ; Li Jia2 ; Li Jingya2 ; Feng Bainian 1
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2016-09
卷号	36 期号:9 页码:2142-2149
关键词	PTP1B SHP2 aromatic amide derivatives inhibitors
ISSN号	0253-2786
DOI	10.6023/cjoc201603045
文献子类	Article
英文摘要	To explore the chemical space of protein tyrosine phosphatase 1B (PTP1B) inhibitors by changing bis-aromatic amide moiety into aromatic amide moiety, a series of aromatic amide derivatives were designed, synthesized and their biological activities were evaluated against PTP1B and Scr homology-2 domain containing protein tyrosine phosphatase-2 (SHP2). Among them, compound 3c displayed moderate inhibitory activity with IC50 of (5.13 +/- 0.21) mu mol/L against PTP1B and showed two times selectivity for other related PTPs. Interestingly, compound 12 [IC50=(7.47 +/- 1.26) mu mol/L] showed moderate inhibitory activity against SHP2 and 2-fold selectivity against PTP1B, T-cell protein tyrosine phosphatase (TCPTP) or Src homology-2 domain containing protein tyrosine phosphatase-1 (SHP1) respectively, and offered a novel scaffold to develop new SHP2 inhibitors.
资助项目	National Natural Science Foundation of China[21472069] ; State Key Laboratory of Drug Research[SEMM1302KF-05]
WOS关键词	OLEANOLIC ACID ; INHIBITORS ; PTP1B
WOS研究方向	Chemistry
语种	中文
CSCD记录号	CSCD:5821608
出版者	SCIENCE PRESS
WOS记录号	WOS:000387095600014
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275904]
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	Li Jingya; Feng Bainian
作者单位	1.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Wang Wenlong,Luo Huan,Gao Ya,et al. Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(9):2142-2149.
APA	Wang Wenlong.,Luo Huan.,Gao Ya.,Gao Lixin.,Sheng Li.,...&Feng Bainian.(2016).Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(9),2142-2149.
MLA	Wang Wenlong,et al."Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.9(2016):2142-2149.