Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B

doi:10.5012/bkcs.2012.33.5.1505

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	Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B
	Chen, Zhen-Hua 1; Sun, Liang-Peng 1; Zhang, Wei 2; Shen, Qiang 2; Gao, Li-Xin 2; Li, Jia2 ; Piao, Hu-Ri 1
刊名	BULLETIN OF THE KOREAN CHEMICAL SOCIETY
	2012-05-20
卷号	33 期号:5 页码:1505-1508
关键词	Chalcone Protein tyrosine phosphatase 1B Inhibitor SAR
ISSN号	0253-2964
DOI	10.5012/bkcs.2012.33.5.1505
文献子类	Article
英文摘要	Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound (4) was first observed to have moderate inhibitory activity against PTP1B with an IC50 value of 13.72 +/- 1.53 mu M. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound (4) as the lead compound. Compound 4I (IC50 = 3.12 +/- 0.18 mu M) was 4.4-fold more potent than the lead compound 4 (IC50 = 13.72 +/- 1.53 mu M), and more potent than the positive control, ursolic acid (IC50=3.40 +/- 0.21 mu M). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
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	INSULIN-RECEPTOR ; SIGNAL-TRANSDUCTION ; DISCOVERY ; OBESITY ; SENSITIVITY ; CANCER ; SERIES ; PTP1B ; ACID ; MICE
WOS研究方向	Chemistry
语种	英语
出版者	KOREAN CHEMICAL SOC
WOS记录号	WOS:000304432100013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278074]
专题	国家新药筛选中心药物安全性评价中心
通讯作者	Li, Jia
作者单位	1.Yanbian Univ, Coll Pharm, Key Lab Nat Resources & Funct Mol Changbai Mt, Affiliated Minist Educ, Yanji 133002, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Chen, Zhen-Hua,Sun, Liang-Peng,Zhang, Wei,et al. Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B[J]. BULLETIN OF THE KOREAN CHEMICAL SOCIETY,2012,33(5):1505-1508.
APA	Chen, Zhen-Hua.,Sun, Liang-Peng.,Zhang, Wei.,Shen, Qiang.,Gao, Li-Xin.,...&Piao, Hu-Ri.(2012).Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B.BULLETIN OF THE KOREAN CHEMICAL SOCIETY,33(5),1505-1508.
MLA	Chen, Zhen-Hua,et al."Synthesis and Biological Evaluation of Heterocyclic Ring-substituted Chalcone Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B".BULLETIN OF THE KOREAN CHEMICAL SOCIETY 33.5(2012):1505-1508.