CAS: 51264-14-3; N-(4-(Acridin-9-Ylamino)-3-Methoxyphenyl)Methanesulfonamide

该化合物是一种炭疽衍生物,是一种合成化合物,主要用作癌症治疗中的抗肾病剂,被归类为一种中间添加剂,这意味着它可以在DNA基配方之间插入,干扰复制和转录过程,最终导致细胞死亡.氨酸盐展示了各种类型的癌症,特别是血液恶性肿瘤的多种活动.氨酸盐因其在癌症细胞中诱发流行性中毒的能力而闻名,使其成为化疗疗治疗中的宝贵工具.在物理特性方面,氨酸盐通常被作为黄色至橙色晶体固态,它溶于有机溶剂,但水溶性有限.其行动机制涉及抑制二号异构体,这是对DNA在复制过程中不摇动至关重要的酶.虽然有效,但氨酸盐还能够产生副作用,包括宫内压和心毒性,因此在治疗过程中需要仔细监测.

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9-Chloroacridine N-(4-amino-3-methoxyphenyl)methanesulfonamide methylthiol N(1')-(methylsulfonyl)-N(4')-(9-acridynyl)-3'-methoxy-2',5'-cyclohexadiene-1',4'-diimineN-(4-amino-3-methoxyphenyl)methanesulfonamide 4-[2-(Acridin-9-ylsulfanyl)-1-(carboxymethyl-carbamoyl)-ethylcarbamoyl]-2-amino-butyric acid

合成工艺路线路线简述

    9-氯吖啶置于盐酸,三乙胺,Tin(Ll) Chloride体系中,用 乙醇,二氯甲烷,氯仿,水 作为反应溶剂,化学反应 18.0H,反应生成 安啶
    参考文献:一种具有肿瘤响应性释放药物的化合物或其药 用盐及其制备,应用
    标题:一种具有肿瘤响应性释放药物的化合物或其药 用盐及其制备,应用
    摘要:一种具有肿瘤响应性释放药物的化合物或其药用盐及其制备,应用,属于药物靶向释放技术领域,其结构式如下:本发明设计,合成一种新型肿瘤细胞敏感性化合物,其在正常生理环境中能够稳定存在,进入肿瘤细胞后,在肿瘤细胞内高浓度谷胱甘肽环境下能够发生串联反应从而释放出安吖啶药物,可用于制备新型靶向抗肿瘤药物.此外,本发明所述化合物的制备方法具有操作简便,条件温和,反应收率高等特点.

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    专利信息


    专利号:US-2004242897-A1
    优先权日:2002-07-31
    标题 :Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    专利号:WO-2004011474-A1
    优先权日:2002-07-31
    标题:Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
    权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-6653468-B1
    优先权日:2002-07-31
    标 题 :Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
    权利人:ISIS PHARMACEUTICALS INC
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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    主要参考文献


    1: Jangir DK, Kundu S, Mehrotra R. Role of minor groove width and hydration pattern on amsacrine interaction with DNA. PLoS One. 2013 Jul 29;8(7):e69933. doi: 10.1371/journal.pone.0069933. Print 2013.
    2: Krejci M, Doubek M, Dusek J, Brychtova Y, Racil Z, Navratil M, Tomiska M, Horky O, Pospisilova S, Mayer J. Combination of fludarabine, amsacrine, and cytarabine followed by reduced-intensity conditioning and allogeneic hematopoietic stem cell transplantation in patients with high-risk acute myeloid leukemia. Ann Hematol. 2013 Jun 1. [Epub ahead of print] doi: 10.1200/JCO.2012.46.4743. Epub 2013 Apr 29. doi: 10.3109/10428194.2012.713479. Epub 2012 Sep 8. doi: 10.1016/j.jphotobiol.2012.05.005. Epub 2012 May 18. doi: 10.1021/bi201159b. Epub 2012 Feb 10.
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    合成参考文献


    参考文献:10.1002/cncr.26190
    摘要:Cooper TM, Franklin J, Gerbing RB, Alonzo TA, Hurwitz C, Raimondi SC, Hirsch B, Smith FO, Mathew P, Arceci RJ, Feusner J, Iannone R, Lavey RS, Meshinchi S, Gamis A. AAML03P1, a pilot study of the safety of gemtuzumab ozogamicin in combination with chemotherapy for newly diagnosed childhood acute myeloid leukemia: a report from the Children's Oncology Group. Cancer. 2012 Feb 01;118(3):761–9. doi: 10.1002/cncr.26190.
    参考文献:10.1007/s15010-011-0158-9
    摘要:Björkholm M, Kalin M, Grane P, Celsing F. Long-term treatment of invasive sinus, tracheobroncheal, pulmonary and intracerebral aspergillosis in acute lymphoblastic leukaemia. Infection. 2012 Feb;40(1):81–5. doi: 10.1007/s15010-011-0158-9.
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