CAS: 950762-95-5; N-Hydroxy-1-(4-Methoxybenzyl)-1H-Indole-6-Carboxamide

该化合物是一个小分子,有选择地抑制蛋白质直流CK2 (casin kinase 2) .该化合物的特点是能够干扰CK2的活动,在细胞扩散,存活和吸附性等各种细胞过程中发挥着关键作用.PCI-34051对CK2的抑制作用进行了研究,以了解其潜在的治疗用途,特别是在癌症治疗方面,因为CK2经常在各种肿瘤中表达过量.该化合物的特点是其与CK2酶的具体结合性,导致对信号路径的下游影响.此外,PCI-34051在临床前研究中对它的功效和安全特征进行了评估,突出其作为定向治疗的潜力.与许多小分子一样,其溶性,稳定性和生物利用率是影响其药理特性和治疗潜力的重要因素.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

PCI-34051 indole-6-carboxylic acid methyl ester p-Methoxybenzyl bromide

合成工艺路线路线简述

    📜Methyl 1-(4-Methoxybenzyl)-1H-Indole-6-Carboxylate置于sodium Hydroxide,羟胺,盐酸体系中,用 四氢呋喃,甲醇,水 作为反应溶剂,化学反应 1.0H,以84%的收率获得产物pci 34051; N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺
    参考文献: Indole Derivatives As Inhibitors Of Histone Deacetylase[fr] Dérivés D'Indole En Tant Qu'Inhibiteurs De L'Histone Désacétylase
    标题: Indole Derivatives As Inhibitors Of Histone Deacetylase[fr] Dérivés D'Indole En Tant Qu'Inhibiteurs De L'Histone Désacétylase

    海关参考信息

    专利信息


    专利号:US-11285169-B2
    优先权日:2013-03-13
    标题 :Methods for modulating chemotherapeutic cytotoxicity
    发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R
    权利人:US HEALTH
    摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

    专利号:US-11801251-B2
    优先权日:2015-11-03
    标 题 :Selective HDAC8 inhibitors and their uses
    发明人:MEYER-ALMES FRANZ-JOSEF; MEYNERS CHRISTIAN; KLEINSCHEK ALEXANDER; HAUS PATRICIA
    权利人:HOCHSCHULE DARMSTADT
    摘要:The present invention relates to small molecule compounds based on benzopyrimido- or benzoimidazo-thiazin-imine as well as their (synthesis) intermediates and their use as HDAC inhibitors, in particular HDAC8 inhibitors. The present invention also relates to the use of said compounds in the treatment of cancer and as therapeutic agents for eukaryotic parasites and respective methods of treatment.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Chen X, Ding X, Fang J, Mao C, Gong X, Zhang Y, Zhang N, Yan F, Lou Y, Chen Z, Ding W, Ma Z. Natural Derivatives of Selective HDAC8 Inhibitors with Potent in Vivo Antitumor Efficacy against Breast Cancer. J Med Chem. 2024 Aug 7. doi: 10.1021/acs.jmedchem.4c01438. Epub ahead of print. 67(15):12784-12806. doi: 10.1021/acs.jmedchem.4c00761. Epub 2024 Jul 1.
    108:129810. doi: 10.1016/j.bmcl.2024.129810. Epub 2024 May 22.
    4: Fukuda M, Fujita Y, Hino Y, Nakao M, Shirahige K, Yamashita T. Inhibition of HDAC8 Reduces the Proliferation of Adult Neural Stem Cells in the Subventricular Zone. Int J Mol Sci. 2024 Feb 22;25(5):2540. doi: 10.3390/ijms25052540.

    合成参考文献


    参考文献:10.1186/s12964-018-0231-4
    摘要:Vanaja GR, Ramulu HG, Kalle AM. Overexpressed HDAC8 in cervical cancer cells shows functional redundancy of tubulin deacetylation with HDAC6. Cell Communication and Signaling. 2018 May 02;16(1):20. doi: 10.1186/s12964-018-0231-4.
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