Design and synthesis of aryloxypropanolamine as beta(3)-adrenergic receptor antagonist in cancer and lipolysis

doi:10.1016/j.ejmech.2018.03.032

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	Design and synthesis of aryloxypropanolamine as beta(3)-adrenergic receptor antagonist in cancer and lipolysis
	Jin, Jiyu 4; Miao, Chunxiao 1; Wang, Zhilong 2; Zhang, Wanli 1; Zhang, Xiongwen 1; Xie, Xin2,3 ; Lu, Wei 4
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2018-04-25
卷号	150 页码:757-770
关键词	beta-Adrenergic receptor Antagonist Cancer Lipolysis and cachexia
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2018.03.032
文献子类	Article
英文摘要	beta-adrenergic receptors (beta-ARs) are broadly distributed in various tissues and regulate a panel of important physiological functions and disease states including cancer. Above all, beta(3)-adrenergic receptor (beta(3)-AR) plays a significant role in regulating lipolysis and thermogenesis in adipose tissue. In this study, we designed and synthesized a series of novel L-748,337 derivatives as selective human beta(3)-AR antagonists. Among all the tested L-748,337 analogs, compound 23d was found to display 23-fold more potent beta(3)-AR antagonist activity (EC50 = 0.5117 nM) than L-748,337 (EC50 = 11.91 nM). In vivo, compound 23d could alleviate weight loss and inhibit tumor growth in C26 tumor cachexia animal model. (C) 2018 Elsevier Masson SAS. All rights reserved.
WOS关键词	MICE ; METASTASIS ; CACHEXIA ; SWITCH
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000430891400054
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279794]
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	Zhang, Xiongwen; Xie, Xin; Lu, Wei
作者单位	1.East ChinaNormal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China 4.East China Normal Univ, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai, Peoples R China;
推荐引用方式 GB/T 7714	Jin, Jiyu,Miao, Chunxiao,Wang, Zhilong,et al. Design and synthesis of aryloxypropanolamine as beta(3)-adrenergic receptor antagonist in cancer and lipolysis[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,150:757-770.
APA	Jin, Jiyu.,Miao, Chunxiao.,Wang, Zhilong.,Zhang, Wanli.,Zhang, Xiongwen.,...&Lu, Wei.(2018).Design and synthesis of aryloxypropanolamine as beta(3)-adrenergic receptor antagonist in cancer and lipolysis.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,150,757-770.
MLA	Jin, Jiyu,et al."Design and synthesis of aryloxypropanolamine as beta(3)-adrenergic receptor antagonist in cancer and lipolysis".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 150(2018):757-770.