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作者:

Zhou, Yumei (Zhou, Yumei.) | Cui, Huaqing (Cui, Huaqing.) | Yu, Xiaoming (Yu, Xiaoming.) | Peng, Tao (Peng, Tao.) | Wang, Gang (Wang, Gang.) | Wen, Xiaoxue (Wen, Xiaoxue.) | Sun, Yunbo (Sun, Yunbo.) | Liu, Shuchen (Liu, Shuchen.) | Zhang, Shouguo (Zhang, Shouguo.) | Hu, Liming (Hu, Liming.) (学者:胡利明) | Wang, Lin (Wang, Lin.)

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摘要:

A series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1-3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration) values at the micromolar level. The preliminary structure-activity relationships were analyzed and the binding features of compound 7e (IC50 3.81 mu M) was predicted using the CDOCKER program. The results of this research could provide informative guidance for further optimizing benzofuran derivatives as potent SIRT2 inhibitors.

关键词:

benzofuran selective SIRT2 inhibitor sulfone sulfoxide

作者机构:

  • [ 1 ] [Zhou, Yumei]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 2 ] [Hu, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 3 ] [Wang, Lin]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 4 ] [Zhou, Yumei]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 5 ] [Peng, Tao]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 6 ] [Wang, Gang]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 7 ] [Wen, Xiaoxue]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 8 ] [Sun, Yunbo]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 9 ] [Liu, Shuchen]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 10 ] [Zhang, Shouguo]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 11 ] [Wang, Lin]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China
  • [ 12 ] [Zhou, Yumei]Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China
  • [ 13 ] [Cui, Huaqing]Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China
  • [ 14 ] [Yu, Xiaoming]Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China
  • [ 15 ] [Zhou, Yumei]Peking Union Med Coll, Beijing 100050, Peoples R China
  • [ 16 ] [Cui, Huaqing]Peking Union Med Coll, Beijing 100050, Peoples R China
  • [ 17 ] [Yu, Xiaoming]Peking Union Med Coll, Beijing 100050, Peoples R China

通讯作者信息:

  • 胡利明

    [Hu, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China;;[Wang, Lin]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China;;[Zhang, Shouguo]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China;;[Wang, Lin]Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China

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来源 :

MOLECULES

ISSN: 1420-3049

年份: 2017

期: 8

卷: 22

4 . 6 0 0

JCR@2022

ESI学科: CHEMISTRY;

ESI高被引阀值:127

中科院分区:3

被引次数:

WoS核心集被引频次: 9

SCOPUS被引频次: 7

ESI高被引论文在榜: 0 展开所有

万方被引频次:

中文被引频次:

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