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首页> 外文期刊>RSC Advances >Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors
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Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors

机译：新型螺环旋转胞嘧啶衍生物作为赖氨酸特异性去甲基酶1（LSD1）抑制剂

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摘要

Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors via conformational restriction using spiro ring systems. A simple, direct spirocyclic analog of tranylcypromine (compounds 8a and 8b) was shown to be a 28- to 129-fold more potent inhibitor of LSD1 enzyme compared to tranylcypromine. Further incorporation of various substituted benzyl groups to the amino group resulted in a suite of 2',3'-dihydrospiro[cyclopropane-1,1'-inden]-2-amines that are potent LSD1 inhibitors with excellent selectivity profiles (e.g. 14a, 15b, 16a, 19a and 20b) against closely related enzymes such as MAO-A, MAO-B, and LSD2.
机译：在此，我们描述了通过使用螺环系统的构象限制来描述新型旋转胞苷基LSD1抑制剂的设计，合成和生物学评价。 与邻邻苯甲酰胞嘧啶相比，替苯甲酰胞丙氨酸（化合物8A和8B）的简单直接螺旋环（化合物8A和8B）的LSD1酶的浓度抑制剂的28至129倍。 进一步掺入氨基中的各种取代苄基导致套2'，3'-二氢哌啶（环丙烷-1,1'-Inden] -2-胺，其是具有优异的选择性谱的有效LSD1抑制剂（例如14A， 15B，16A，19A和20B）针对密切相关的酶，例如MAO-A，MAO-B和LSD2。

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  • 来源
    《RSC Advances》 |2018年第3期|共11页
  • 作者

    Shi Ying; Wu Yan-Ran; Su Ming-Bo; Shen Dong-Hao; Gunosewoyo Hendra; Yang Fan; Li Jia; Tang Jie; Zhou Yu-Bo; Yu Li-Fang;

  • 作者单位

    East China Normal Univ Sch Chem &

    Mol Engn Shanghai Engn Res Ctr Mol Therapeut &

    New Drug De 3663 North Zhongshan Rd Shanghai 200062 Peoples R China;

    East China Normal Univ Sch Chem &

    Mol Engn Shanghai Engn Res Ctr Mol Therapeut &

    New Drug De 3663 North Zhongshan Rd Shanghai 200062 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med Natl Ctr Drug Screening CAS Key Lab Receptor Res 189 Guo Shou Jing Rd Shanghai 201203 Peoples R China;

    East China Normal Univ Sch Chem &

    Mol Engn Shanghai Engn Res Ctr Mol Therapeut &

    New Drug De 3663 North Zhongshan Rd Shanghai 200062 Peoples R China;

    Curtin Univ Fac Hlth Sci Sch Pharm Bentley WA 6102 Australia;

    East China Normal Univ Sch Chem &

    Mol Engn Shanghai Engn Res Ctr Mol Therapeut &

    New Drug De 3663 North Zhongshan Rd Shanghai 200062 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med Natl Ctr Drug Screening CAS Key Lab Receptor Res 189 Guo Shou Jing Rd Shanghai 201203 Peoples R China;

    East China Normal Univ Sch Chem &

    Mol Engn Shanghai Key Lab Green Chem &

    Chem Proc 3663 North Zhongshan Rd Shanghai 200062 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med Natl Ctr Drug Screening CAS Key Lab Receptor Res 189 Guo Shou Jing Rd Shanghai 201203 Peoples R China;

    East China Normal Univ Sch Chem &

    Mol Engn Shanghai Engn Res Ctr Mol Therapeut &

    New Drug De 3663 North Zhongshan Rd Shanghai 200062 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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