Design and synthesis of aryloxypropanolamine as beta(3)-adrenergic receptor antagonist in cancer and lipolysis
文献类型：期刊论文
| 作者 | Jin, Jiyu4; Miao, Chunxiao1; Wang, Zhilong2; Zhang, Wanli1; Zhang, Xiongwen1; Xie, Xin2,3 ; Lu, Wei4
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 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 |
| WOS记录号 | WOS:000430891400054 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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