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Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor

文献类型：期刊论文

作者Jiang, Cheng-Shi1; Zhou, Rong2; Gong, Jing-Xu1; Chen, Li-Li1; Kurtan, Tibor3; Shen, Xu1,2; Guo, Yue-Wei1
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
出版日期2011-02-15
卷号21期号:4页码:1171-1175
关键词Macrolide (R)-De-O-methyllasiodiplodin Mineralocorticoid receptor Antagonist Ring-closing-metathesis reaction
ISSN号0960-894X
DOI10.1016/j.bmcl.2010.12.101
文献子类Article
英文摘要Macrolide (R)-de-O-methyllasiodiplodin (1), discovered to be a potent nonsteroidal antagonist of the mineralocorticoid receptor (MR), was synthesized via an efficient method and evaluated for MR antagonistic activity together with its analogs. Among all the tested compounds, compounds 18a, 18b and 18c, exhibited more potent antagonistic activity against MR with IC50 values ranging from 0.58 to 1.11 mu M. Generally, it was obviously demonstrated that acetylation at phenolic hydroxyl groups and the ring size in analogs of 1 were very important for MR antagonist activity. (c) 2010 Elsevier Ltd. All rights reserved.
WOS关键词RING-CLOSING-METATHESIS ; POTENT ; METABOLITES ; MACROLIDE ; BIOLOGY ; (R)-(+)-LASIODIPLODIN ; LASIODIPLODIN ; CONSTITUENTS ; ALDOSTERONE ; CONGENERS
资助项目National S & T Major Project[2009ZX09301-001] ; National S & T Major Project[2009ZX09103-060] ; National Marine 863 Programme for Druggability Evaluation[00000000] ; Natural Science Foundation of China[30730108] ; Natural Science Foundation of China[40976048] ; Natural Science Foundation of China[81072572] ; STCSM[09ZR1438000] ; STCSM[10540702900] ; CAS[SIMM0907KF-09] ; CAS[KSCX2-YW-R-18]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000286972400018
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/278603]  
专题天然药物化学研究室
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Gong, Jing-Xu
作者单位1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.E China Univ Sci & Technol, Shanghai 200237, Peoples R China;
3.Univ Debrecen, Dept Organ Chem, H-4010 Debrecen, Hungary
推荐引用方式
GB/T 7714		 Jiang, Cheng-Shi,Zhou, Rong,Gong, Jing-Xu,et al. Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(4):1171-1175.
APA Jiang, Cheng-Shi.,Zhou, Rong.,Gong, Jing-Xu.,Chen, Li-Li.,Kurtan, Tibor.,...&Guo, Yue-Wei.(2011).Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(4),1171-1175.
MLA Jiang, Cheng-Shi,et al."Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.4(2011):1171-1175.

入库方式： OAI收割

来源：上海药物研究所

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