Identification of 1, 4-Dihydrothieno[3 ', 2 ':5, 6] thiopyrano [4, 3-c]pyrazole Derivatives as Human 5-Lipo-oxygenase Inhibitors

doi:10.1111/cbdd.12356

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	Identification of 1, 4-Dihydrothieno[3 ', 2 ':5, 6] thiopyrano [4, 3-c]pyrazole Derivatives as Human 5-Lipo-oxygenase Inhibitors
	Hu, Jianshu 1; Zhu, Wei 1; Meng, Hu 1; Liu, Ying 1; Wang, Xin 2,3; Hu, Chun 2,3
刊名	CHEMICAL BIOLOGY & DRUG DESIGN
	2014-12-01
卷号	84 期号:6 页码:642-647
关键词	Bioassay Cross-reactivity Human 5-lipo-oxygenase Inhibitors Molecular Docking Synthesis
ISSN号	1747-0277
DOI	10.1111/cbdd.12356
英文摘要	A series of novel 1,4-dihydrothieno[3,2:5,6]thiopyrano[4,3-c]-pyrazole-3-carboxamide derivatives were synthesized and evaluated for their inhibitory activity to human 5-lipo-oxygenase (5-LOX). Compound 7c was found to exhibit significant inhibition to human 5-LOX with IC50 value of 5.7 +/- 0.9m. Compound 7c was further studied using molecular docking in order to delineate its structure-activity relationship and to gain insight into the design of effective 5-LOX inhibitors.
语种	英语
出版者	WILEY-BLACKWELL
WOS记录号	WOS:000345219600002
内容类型	期刊论文
源URL	[http://ir.iccas.ac.cn/handle/121111/51045]
专题	中国科学院化学研究所
通讯作者	Liu, Ying
作者单位	1.Peking Univ, Beijing Natl Lab Mol Sci, Coll Chem & Mol Engn, State Key Lab Struct Chem Unstable & Stable Speci, Beijing 100871, Peoples R China 2.Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China 3.Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China
推荐引用方式 GB/T 7714	Hu, Jianshu,Zhu, Wei,Meng, Hu,et al. Identification of 1, 4-Dihydrothieno[3 ', 2 ':5, 6] thiopyrano [4, 3-c]pyrazole Derivatives as Human 5-Lipo-oxygenase Inhibitors[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2014,84(6):642-647.
APA	Hu, Jianshu,Zhu, Wei,Meng, Hu,Liu, Ying,Wang, Xin,&Hu, Chun.(2014).Identification of 1, 4-Dihydrothieno[3 ', 2 ':5, 6] thiopyrano [4, 3-c]pyrazole Derivatives as Human 5-Lipo-oxygenase Inhibitors.CHEMICAL BIOLOGY & DRUG DESIGN,84(6),642-647.
MLA	Hu, Jianshu,et al."Identification of 1, 4-Dihydrothieno[3 ', 2 ':5, 6] thiopyrano [4, 3-c]pyrazole Derivatives as Human 5-Lipo-oxygenase Inhibitors".CHEMICAL BIOLOGY & DRUG DESIGN 84.6(2014):642-647.