synthesisandcelldivisioncycle25bphosphataseandproteintyrosinephosphatase1binhibitoryactivityevaluationofnovel36disubstitutedtriazolothiadiazolederivatives

doi:10.6023/cjoc201607030

	synthesisandcelldivisioncycle25bphosphataseandproteintyrosinephosphatase1binhibitoryactivityevaluationofnovel36disubstitutedtriazolothiadiazolederivatives
	Li YJ(李英俊)2; Li JY(李继阳)2; Peng LN(彭立娜)2; Gao LX(高立信)3; Jin K(靳焜)1; Sheng L(盛丽)3; Zhang N(张楠)2; Wang SY(王思远)2; Li J(李佳)3
刊名	chinesejournaloforganicchemistry
	2017
卷号	37 期号:2 页码:485
关键词	BIOLOGICAL-ACTIVITIES ANALOGS ACID triazolothiadiazole benzimidazole arylsulfonyl synthesis Cdc25B and PTP1B inhibitors
ISSN号	0253-2786
DOI	10.6023/cjoc201607030
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]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/286765]
专题	中国科学院上海药物研究所
作者单位	1.大连理工大学 2.辽宁师范大学 3.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Li YJ,Li JY,Peng LN,et al. synthesisandcelldivisioncycle25bphosphataseandproteintyrosinephosphatase1binhibitoryactivityevaluationofnovel36disubstitutedtriazolothiadiazolederivatives[J]. chinesejournaloforganicchemistry,2017,37(2):485.
APA	李英俊.,李继阳.,彭立娜.,高立信.,靳焜.,...&李佳.(2017).synthesisandcelldivisioncycle25bphosphataseandproteintyrosinephosphatase1binhibitoryactivityevaluationofnovel36disubstitutedtriazolothiadiazolederivatives.chinesejournaloforganicchemistry,37(2),485.
MLA	李英俊,et al."synthesisandcelldivisioncycle25bphosphataseandproteintyrosinephosphatase1binhibitoryactivityevaluationofnovel36disubstitutedtriazolothiadiazolederivatives".chinesejournaloforganicchemistry 37.2(2017):485.