📜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
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.
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.