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Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression  期刊论文  

  • 编号:
    560112f7-98e7-423a-bbba-42626e9b1ea1
  • 作者:
    Qiu, Ruomeng[1];Shi, Wenli[2];Cai, Ting[2];Pei, Siyu[2];Tang, Ting[1];Huang, Yafei[1];Wang, Huan[1];Shao, Liming[1];Qiu, Ju[2];Wang, Yonghui(王永辉)*[1]
  • 地址:

    [1]Fudan Univ, Sch Pharm, Dept Med Chem, 826 Zhangheng Rd, Shanghai 201203, Peoples R China;

    [2]Univ Chinese Acad Sci, Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Hlth Sci, Shanghai 200031, Peoples R China

  • 语种:
    English
  • 期刊:
    MEDCHEMCOMM ISSN:2040-2503 2016 年 7 卷 12 期 (2344 - 2348)
  • 收录:
  • 摘要:

    A series of N-biaryl amides for Th17 cell phenotypic screening were designed and quickly prepared by microwave-assisted solid-phase organic synthesis. The structure-activity relationship of the three regions of the amides was explored and potent small molecular inhibitors that suppress IL-17A production in mouse Th17 cells were identified. Compound 6h showed excellent suppression of IL-17A with an IC50 of 13 nM, which can be employed as a chemical tool for target identification and Th17 cell-related biological studies.

  • 推荐引用方式
    GB/T 7714:
    Qiu Ruomeng,Shi Wenli,Cai Ting, et al. Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression [J].MEDCHEMCOMM,2016,7(12):2344-2348.
  • APA:
    Qiu Ruomeng,Shi Wenli,Cai Ting,Pei Siyu,&Wang Yonghui.(2016).Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression .MEDCHEMCOMM,7(12):2344-2348.
  • MLA:
    Qiu Ruomeng, et al. "Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression" .MEDCHEMCOMM 7,12(2016):2344-2348.
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