國家衛生研究院 NHRI:Item 3990099045/9612
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    题名: A new application of parallel synthesis strategy for discovery of amide-linked small molecules as potent chondroprotective agents in TNF-alpha-stimulated chondrocytes
    其它题名: A new application of parallel synthesis strategy for discovery of amide-linked small molecules as potent chondroprotective agents in TNF-α-stimulated chondrocytes
    作者: Lee, CC;Lo, Y;Ho, LJ;Lai, JH;Lien, SB;Lin, LC;Chen, CL;Chen, TC;Liu, FC;Huang, HS
    贡献者: Institute of Cellular and Systems Medicine
    摘要: As part of an effort to profile potential therapeutics for the treatment of inflammation-related diseases, a diversity of amide-linked small molecules was synthesized by using parallel synthesis strategy. Moreover, these new compounds were also evaluated for their inhibitory effects on nitric oxide (NO) by using tumor necrosis factor alpha (TNF-alpha)-induced inflammatory responses in chondrocytes. Among the tested compounds, N-(3-chloro-4-fluorophenyl)-2-hydroxybenzamide (HS-Ck) was the most potent inhibitor of NO production and inducible nitric oxide synthase (iNOS) expression in TNF-alpha-stimulated chondrocytes. In addition, our biological results indicated that HS-Ck might suppress the expression levels of iNOS and matrix metalloproteinases-13 (MMP-13) activities through downregulating the activation of nuclear factor kappa B (NF-kappaB) and signal transducer and activator of transcription 3 (STAT-3) transcriptional factors. Therefore, the parallel synthesis was successful used to develop a new class of potential anti-inflammatory agents as chondroprotective candidates for the treatment of osteoarthritis.
    日期: 2016-03-10
    關聯: PLoS ONE. 2016 Mar 10;11(3):Article number e0149317.
    Link to: http://dx.doi.org/10.1371/journal.pone.0149317
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1932-6203&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000371993000010
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84962556853
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