CAS: 934541-31-8; 5-(3-(Ethylsulfonyl)Phenyl)-3,8-Dimethyl-N-(1-Methylpiperidin-4-yl)-9H-Pyrido[2,3-B]Indole-7-Carboxamide

该化合物是一种化学化合物,在制药研究中引起注意,特别是在肿瘤学方面,被归类为小分子抑制剂,具体针对癌症细胞扩散和存活的某些途径.该化合物展示了一种独特的行动机制,可能涉及调节特定蛋白相互作用或对肿瘤生长至关重要的酶活动.TAK-901的特点是其结构特征,包括有助于其生物活动和溶液特征的特定功能组.在临床前的研究中,它显示出抑制各种癌症模型肿瘤生长的希望,导致对临床环境中肿瘤的功效和安全性进行持续调查.与许多调查药物一样,其整系列的药性动力学,药用动力学和潜在副作用仍在评估中,因此它成为目标癌症疗法进一步研究的对象.

结构式图片

物理性质

MSDS等安全信息

上下游产品

4-Amino-1-methylpiperidine 5-[3-(ethylsulfonyl)phenyl]-3,8-dimethyl-9H-pyrido[2,3-b]indole-7-carboxylic acid 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide monohydr°Chloride 2,3-dichloro-5-trifluoromethyl-6-methylnitrobenzene

合成工艺路线路线简述

  • 41838-46-4 + 934542-76-4 = 934541-31-8
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide,Dichloromethane; 30 Min,Rt1.2 Reagents: Sodium Bicarbonate; Basified
    标题:Pyrido[2,3-B]Indole Derivatives As Kinase Inhibitors And Their Preparation And Use In The Treatment Of Diseases
    参考文献:World Intellectual Property Organization]

    41838-46-4 + 934542-76-4 = 934541-31-8
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide,Dichloromethane; 30 Min,Rt
    标题:Polymorphs Of 5-(3-(Ethylsulfonyl)Phenyl)-3,8-Dimethyl-N-(1-Methylpiperidin-4-Yl)-9H-Pyrido[2,3-B]Indole-7-Carboxamide For Disease Treatment
    参考文献:World Intellectual Property Organization]

    = 934541-31-8 [标题:Reaction Conditions
    标题:Polymorphs Of 5-(3-(Ethylsulfonyl)Phenyl)-3,8-Dimethyl-N-(1-Methylpiperidin-4-Yl)-9H-Pyrido[2,3-B]Indole-7-Carboxamide And Methods Of Use Therefor
    参考文献:United States]

    = 934541-31-8 [标题:Reaction Conditions
    标题:Polymorphs Of Hydrochloride Salt Of 5-(3-(Ethylsulfonyl)Phenyl)-3,8-Dimethyl-N-(1-Methylpiperidin-4-Yl)-9H-Pyrido[2,3-B]Indole-7-Carboxamide To Treat A Diseases Involving Kinase Activity
    参考文献:World Intellectual Property Organization]

    41838-46-4 + 934542-76-4 = 934541-31-8
    反应条件:1.1 Reagents: 1-[bis(Dimethylamino)Methylene]-1H-Benzotriazolium Hexafluorophosphate(1-) 3-Oxi... Solvents: N-Methyl-2-Pyrrolidone; 2 H,20 - 30 °C1.2 Reagents: Potassium Hydroxide Solvents: Water; Rt
    标题:Integrated Cross-Coupling Strategy For An α-Carboline-Based Aurora B Kinase Inhibitor
    作者:Mineno,Masahiro; Sera,Misayo; Ueda,Tsuyoshi; Mizufune,Hideya; Zanka,Atsuhiko; Et Al
    参考文献:Journal Of Organic Chemistry 日期:2015 卷标:80(3) 页码:1564-1568]

    41838-46-4 + 934542-76-4 = 934541-31-8
    反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide,Dichloromethane; 30 Min,Rt
    标题:Preparation Of Pyridoindoles As Kinase Inhibiting Compounds For Treating And Preventing Kinase-Associated Diseases
    参考文献:World Intellectual Property Organization]

    41838-46-4 + 934542-76-4 = 934541-31-8
    反应条件:1.1 Reagents: Triethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide; 2 D,Rt
    标题:Preparation Of Pyridoindoles As Kinase Inhibitors
    参考文献:United States]

    = 934541-31-8 [标题:Reaction Conditions
    标题:Preparation Of Pyridoindoles As Kinase Inhibiting Compounds For Treating And Preventing Kinase-Associated Diseases
    参考文献:World Intellectual Property Organization
📜5-(3-(乙基磺酰基)苯基)-3,8-二甲基-7-(三氟甲基)-9H-吡啶并[2,3-B]吲哚单乙酸酯置于硫酸,二乙胺,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-)体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 1.0H,反应生成 5-[3-(乙基磺酰基)苯基]-3,8-二甲基-N-(1-甲基-4-哌啶基)-9H-吡啶并[2,3-B]吲哚-7-甲酰胺
参考文献: Kinase Inhibitors[fr] Inhibiteurs De Kinases
标题: Kinase Inhibitors[fr] Inhibiteurs De Kinases

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.

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主要参考文献


1: Rao X, Qiao Z, Yang Y, Deng Y, Zhang Z, Yu X, Guo X. Unveiling Epigenetic Vulnerabilities in Triple-Negative Breast Cancer through 3D Organoid Drug Screening. Pharmaceuticals (Basel). 2024 Feb 8;17(2):225. doi: 10.3390/ph17020225.
2: Ly CY, Pfannenstiel J, Pant A, Yang Z, Fehr AR, Rodzkin MS, Davido DJ. Inhibitors of One or More Cellular Aurora Kinases Impair the Replication of Herpes Simplex Virus 1 and Other DNA and RNA Viruses with Diverse Genomes and Life Cycles. Microbiol Spectr. 2023 Feb 14;11(1):e0194322. doi: 10.1128/spectrum.01943-22. Epub 2022 Dec 20.
3: Krushkal J, Silvers T, Reinhold WC, Sonkin D, Vural S, Connelly J, Varma S, Meltzer PS, Kunkel M, Rapisarda A, Evans D, Pommier Y, Teicher BA. Epigenome- wide DNA methylation analysis of small cell lung cancer cell lines suggests potential chemotherapy targets. Clin Epigenetics. 2020 Jun 25;12(1):93. doi: 10.1186/s13148-020-00876-8.

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摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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