Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives

doi:10.6023/cjoc201607030

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	Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives
	Li Yingjun 1; Li Jiyang 1; Peng Lina 1; Gao Lixin 3; Jin Kun 2; Sheng Li 3; Zhang Nan 1; Wang Siyuan 1; Li Jia3
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2017-02-25
卷号	37 期号:2 页码:485-495
关键词	triazolothiadiazole benzimidazole arylsulfonyl synthesis Cdc25B and PTP1B inhibitors
ISSN号	0253-2786
DOI	10.6023/cjoc201607030
文献子类	Article
英文摘要	A series of new 3,6-disubstituted triazolothiadiazole derivatives 7a similar to 7y containing benzimidazole and arylsulfonyl moities have been synthesized by o-pheny lenediamine and chloroacetic acid as starting materials via multistep reactions. The structures of the intermediates 3, 4, 6 and the target compounds 7 were characterized by H-1 NMR, IR spectra and elemental analysis. All synthesized target compounds were screened for their inhibitory activity against cell division cycle 25B phosphatase (Cdc25B) and protein tyrosine phosphatase 1B (PTP1B). The results show that some of them display significant inhibitory activities against Cdc25B and PTP1B. Among them, compound 7d exhibits the highest inhibitory activity against Cdc25B [ IC50=(7.72 perpendicular to 0.73) mu g/mL] and 7u exhibits the highest inhibitory activity against PTP1B [ IC50=(3.31 perpendicular to 0.57) mu g/mL]. It is noteworthy that compounds 7b, 7d, 7l, 7t and 7u show higher inhibitory activities against Cdc25B and PTP1B. They can be considered as potential Cdc25B and PTP1B inhibitors, and have great application prospects in the treatment of cancers and diabetes.
资助项目	Natural Science Foundation of Liaoning Province[20102126]
WOS关键词	BIOLOGICAL-ACTIVITIES ; ANTICANCER AGENTS ; PTP1B INHIBITORS ; SCAFFOLDS ; ANALOGS ; DESIGN ; MOIETY ; ACID
WOS研究方向	Chemistry
语种	中文
CSCD记录号	CSCD:5947952
出版者	SCIENCE PRESS
WOS记录号	WOS:000397808100022
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272767]
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药物安全性评价中心
通讯作者	Li Yingjun; Li Jia
作者单位	1.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China; 2.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China 3.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	Li Yingjun,Li Jiyang,Peng Lina,et al. Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2017,37(2):485-495.
APA	Li Yingjun.,Li Jiyang.,Peng Lina.,Gao Lixin.,Jin Kun.,...&Li Jia.(2017).Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,37(2),485-495.
MLA	Li Yingjun,et al."Synthesis and Cell Division Cycle 25B Phosphatase and Protein Tyrosine Phosphatase 1B Inhibitory Activity Evaluation of Novel 3,6-Disubstituted Triazolothiadiazole Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 37.2(2017):485-495.