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Issue 12, 2016
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Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression

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Abstract

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.

Graphical abstract: Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression

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Publication details

The article was received on 28 Jul 2016, accepted on 13 Sep 2016, published on 22 Sep 2016 and first published online on 22 Sep 2016


Article type: Research Article
DOI: 10.1039/C6MD00427J
Citation: Med. Chem. Commun., 2016,7, 2344-2348
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    Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression

    R. Qiu, W. Shi, T. Cai, S. Pei, T. Tang, Y. Huang, H. Wang, L. Shao, J. Qiu and Y. Wang, Med. Chem. Commun., 2016, 7, 2344
    DOI: 10.1039/C6MD00427J

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