Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT(1) Selective Antagonists

doi:10.1021/acsmedchemlett.5b00482

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	Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT(1) Selective Antagonists
	Chen, Huayan 1; Yang, Hui 2; Wang, Zhilong 2; Xie, Xin2 ; Nan, Fajun1
刊名	ACS MEDICINAL CHEMISTRY LETTERS
	2016-03
卷号	7 期号:3 页码:335-339
关键词	Cysteinyl leukotrienes CysLT(1) CysLT(2) selective antagonists asthma
ISSN号	1948-5875
DOI	10.1021/acsmedchemlett.5b00482
文献子类	Article
英文摘要	The indole derivative, 34(E)-3-((3-((E)-2-(7-chloroquinolin-2yl)vinyl)phenyl)amino)-3-oxoprop-1-en-1-yl)-7-methoxy-1H-indole-2-carboxylic acid (17k), was identified as a novel and highly potent and selective CysLT(1) antagonist with IC50 values of 0.0059 +/- 0.0011 and 15 +/- 4 mu M for CysLT(1) and CysLT(2), respectively.
资助项目	Ministry of Science and Technology of China[2015CB964503] ; National Natural Science Foundation of China[81425024]
WOS关键词	CYSTEINYL-LEUKOTRIENES ; RECEPTOR ; POTENT ; EXPRESSION ; ASTHMA
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000372042900026
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276119]
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	Xie, Xin; Nan, Fajun
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Chen, Huayan,Yang, Hui,Wang, Zhilong,et al. Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT(1) Selective Antagonists[J]. ACS MEDICINAL CHEMISTRY LETTERS,2016,7(3):335-339.
APA	Chen, Huayan,Yang, Hui,Wang, Zhilong,Xie, Xin,&Nan, Fajun.(2016).Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT(1) Selective Antagonists.ACS MEDICINAL CHEMISTRY LETTERS,7(3),335-339.
MLA	Chen, Huayan,et al."Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT(1) Selective Antagonists".ACS MEDICINAL CHEMISTRY LETTERS 7.3(2016):335-339.