Syntheses of oxysterol receptors'(LXRs) ligands

ZHOU Xiangdong; ZHEN Hui; ZHOU Weishan

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Syntheses of oxysterol receptors'(LXRs) ligands

机译：氧固醇受体（LXRs）配体的合成

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摘要

The LXRs' agonist, 24S,25-epoxycholcstcrol 1, was synthesized stereoselectively (100% d.e.) in 56% overall yield from methyl hyodeoxycholanate 4 in 9 steps with des-mosterol acetate 11 as the key intermediate and the modified Sharpless asymmetric dihydroxylation as the key step. The LXRα subtype selective agonist 5α,6α:24S,25-diepoxycho-lesterol 2 and the novel LXRs' ligand 5β,6β:24S,25-diepo-xycholesterol 3 were also synthesized from 1.

机译：LXRs的激动剂24S，25-epoxycholcstcrol 1由去氧胆甾醇乙酸酯4作为主要中间体，经修饰的Sharpless不对称二羟基化反应以9个步骤立体选择性地（100％de）合成了猪去氧胆酸甲酯4，总收率为56％。关键步骤。 LXRα亚型选择性激动剂5α，6α：24S，25-二乙氧基胆甾醇2和新型LXR's配体5β，6β：24S，25-二乙氧基胆固醇3也由1合成。

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来源
《Chinese science bulletin》 |2003年第3期|p.247-254|共8页
作者
ZHOU Xiangdong; ZHEN Hui; ZHOU Weishan;
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作者单位

Department of Pharmacy, The Third Millitary Medical University, Chongqing 400038, China;

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原文格式 PDF
正文语种 eng
中图分类自然科学现状及发展;
关键词
methyl hyodeoxycholanate; desmosterol acetate; 24S; 25-epoxycholesterol; sharpless catalytic asymmetric dihydoxylation; LXRs' agonists;

机译：猪去氧胆酸甲酯;醋酸去骨甾醇;24S;25-环氧胆固醇;无尖锐的催化不对称二羟化;LXRs激动剂;

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2. The oxysterol receptors lxrα and lxrβ suppress proliferation in the colon [J] . VedinL.-L., GustafssonJ.-A., SteffensenK.R. Molecular Carcinogenesis . 2013,第11期

机译：氧固醇受体lxrα和lxrβ抑制结肠中的增殖
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4. Molecular docking of G. Pentaphyllum to LXRs receptors and agonist screening [C] . Liu Ming, Jieqing Liu, Hu Wenxiang 2011 2nd International Conference on Artificial Intelligence, Management Science and Electronic Commerce . 2011

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5. Syntheses and Evaluations of Bicycloheptylamines and Cyclohexylamines as Sigma-2 Receptor Ligands and Their Potential as Anticancer Agents. [D] . Alamri, Mohammed A. 2017

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6. Structural requirements of ligands for the oxysterol liver X receptors LXRα and LXRβ [O] . Bethany A. Janowski, Michael J. Grogan, Stacey A. Jones, 1999

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7. Regulation of the Aldo-Keto Reductase Gene akr1b7 by the Nuclear Oxysterol Receptor LXRα (Liver X Receptor-α) in the Mouse Intestine: Putative Role of LXRs in Lipid Detoxification Processes [O] . David H. Volle, Joyce J. Repa, Andrzej Mazur, 2004

机译：小鼠肠道核氧巢醇受体LXRα（肝X受体-α）的核氧基酮还原酶基因AKR1B7调节：LXR在脂质排毒过程中的推定作用

Syntheses of oxysterol receptors'(LXRs) ligands

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