Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists

doi:10.1111/cbdd.13184

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	Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists
	Li, Jia1,2,3,4 ; Feng, Yang 5; Li, Huihui 2,3,4; Shu, Shuangjie 2,3,4; Dai, Antao 5; Cai, Xiaoqing 5; Wang, Jiang2,3,4 ; Yang, Dehua3,4,5 ; Ma, Dakota 5; Wang, Ming-Wei3,4,5
刊名	CHEMICAL BIOLOGY & DRUG DESIGN
	2018-07
卷号	92 期号:1 页码:1241-1254
关键词	biaryl amide glucagon receptor antagonist molecular simulation
ISSN号	1747-0277
DOI	10.1111/cbdd.13184
文献子类	Article
英文摘要	A novel series of thiophene-containing biaryl amide glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, 14f and 14h, exhibited good GCGR binding (IC50=6.1 and 4.4m, respectively) and cAMP functional activities (IC50=4.4 and 14.4m, respectively). The possible binding modes of compounds 14f and 14h with GCGR were explored by molecular simulation.
资助项目	National Natural Science Foundation of China[21632008] ; National Natural Science Foundation of China[81620108027] ; National Natural Science Foundation of China[21672231] ; National Natural Science Foundation of China[21472209] ; Major Project of Chinese National Programs for Fundamental Research and Development[2015CB910304] ; SA-SIBS Scholarship Program[00000000] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Shanghai Science and Technology Development Fund[15QA1404400] ; Thousand Talents Program in China[00000000] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12040201] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12040202]
WOS关键词	TYPE-2 DIABETES-MELLITUS ; GLUCOSE ; METABOLISM ; EXCRETION ; AGONISTS
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种	英语
出版者	WILEY
WOS记录号	WOS:000436403500008
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279686]
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化学研究室药物安全性评价中心
通讯作者	Wang, Ming-Wei; Liu, Hong
作者单位	1.China Pharmaceut Univ, Sch Pharm, Nanjing, Jiangsu, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai, Peoples R China; 4.Univ Chinese Acad Sci, Beijing, Peoples R China; 5.Natl Ctr Drug Screening, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Li, Jia,Feng, Yang,Li, Huihui,et al. Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2018,92(1):1241-1254.
APA	Li, Jia.,Feng, Yang.,Li, Huihui.,Shu, Shuangjie.,Dai, Antao.,...&Liu, Hong.(2018).Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists.CHEMICAL BIOLOGY & DRUG DESIGN,92(1),1241-1254.
MLA	Li, Jia,et al."Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists".CHEMICAL BIOLOGY & DRUG DESIGN 92.1(2018):1241-1254.