國家衛生研究院 NHRI:Item 3990099045/15422
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    题名: Analysis of structure–activity relationship of indol-3-yl-N-phenylcarbamic amides as potent STING inhibitors
    作者: Chang, PW;Wang, JY;Wang, WP;Huang, WC;Wu, MH;Song, JS;Chen, LY;Tung, CW;Chi, YH;Ueng, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: A structure–activity relationship (SAR) study of stimulator of interferon gene (STING) inhibition was performed using a series of indol-3-yl-N-phenylcarbamic amides and indol-2-yl-N-phenylcarbamic amides. Among these analogs, compounds 10, 13, 15, 19, and 21 inhibited the phosphorylation of STING and interferon regulatory factor 3 (IRF3) to a greater extent than the reference compound, H-151. All five analogs showed stronger STING inhibition than H-151 on the 2′,3′-cyclic GMP-AMP-induced expression of interferon regulatory factors (IRFs) in a STINGR232 knock-in THP-1 reporter cell line. The half-maximal inhibitory concentration of the most potent compound, 21, was 11.5 nM. The molecular docking analysis of compound 21 and STING combined with the SAR study suggested that the meta- and para-positions of the benzene ring of the phenylcarbamic amide moiety could be structurally modified by introducing halides or alkyl substituents.
    日期: 2023-11-15
    關聯: Bioorganic and Medicinal Chemistry. 2023 Nov 15;95:Article number 117502.
    Link to: http://dx.doi.org/10.1016/j.bmc.2023.117502
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0968-0896&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:001094473000001
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85174729946
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