國家衛生研究院 NHRI:Item 3990099045/11323
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    题名: 5-aroylindoles act as selective histone deacetylase 6 inhibitors ameliorating alzheimer's disease phenotypes
    作者: Lee, HY;Fan, SJ;Huang, FI;Chao, HY;Hsu, KC;Lin, TE;Yeh, TK;Lai, MJ;Li, YH;Huang, HL;Yang, CR;Liou, JP
    贡献者: Institute of Biotechnology and Pharmaceutical Research
    摘要: This paper reports the development of a series of 5-aroylindolyl-substituted hydroxamic acids. N-Hydroxy-4-((5-(4-methoxybenzoyl)-1 H-indol-1-yl)methyl)benzamide (6) has potent inhibitory selectivity against histone deacetylase 6 (HDAC6) with an IC50 value of 3.92 nM. It decreases not only the level of phosphorylation of tau proteins but also the aggregation of tau proteins. Compound 6 also shows neuroprotective activity by triggering ubiquitination. In animal models, compound 6 is able to ameliorate the impaired learning and memory, and it crosses the blood-brain barrier after oral administration. Compound 6 can be developed as a potential treatment for Alzheimer's disease in the future.
    日期: 2018-08-23
    關聯: Journal of Medicinal Chemistry. 2018 Aug 23;61(16):7087-7102.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.8b00151
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000442960800009
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85050635071
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