CAS: 519-23-3; 5,11-Dimethyl-6H-Pyrido[4,3-B]Carbazole

该化合物是一种以其强大的生物活动而闻名的有状[4,3-b]碳氨酸结构的平面藻类化合物,它与DNA具有很强的互缩性,干扰复制和转录过程,使其成为生物化学和药理研究的宝贵工具. 椭圆脂及其衍生物表现出了重要的抗沙素和抗病毒特性,特别是在针对二类异构体酶抑制物的研究中. 它的荧光特性也使得它能够用作核酸研究的探针. 由于它的平面芳香系统, 椭圆石素需要小心处理,以确保稳定性. 化合物主要用于实验性肿瘤学和分子生物学,用于DNA相互作用剂的机械学研究.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

1-[1-acetyl-3-(1,1-di-indol-3-yl-ethyl)-1,4-dihydro-[4]pyridyl]-ethanone carbazole2-(p-methoxbenzyl)-1,2,3,4-tetrahydro-5,11-dimethylpyrido4,3-bcarbazole methyllithium naphthyridin-12-one5-hydroxy-5-methyl-indolo1,2-b2,7naphthyridin-12-one6-benzyl-5,11-dimethyl-6H-pyrido[4,3-b]carbazole 2-benzoyl-1-cyano-1,2-dihydroellipticine 2-Benzenesulfonyl-5,11-dimethyl-2,6-dihydro-1H-pyrido[4,3-b]carbazole-1-carbonitrile 6-methylellipticine

合成工艺路线路线简述

    📜2-碘苯胺置于盐酸,Lithium Chloro-Isopropyl-Magnesium Chloride,Sodium Azide,三氟化硼乙醚,三氟乙酸,Sodium Nitrite体系中,用 四氢呋喃,二氯甲烷,水,均三甲苯 作为反应溶剂,化学反应 12.75H,反应生成 椭圆玫瑰树碱
    参考文献:Preparation Of Polyfunctional Aryl Azides From Aryl Triazenes. A New Synthesis Of Ellipticine,9-Methoxyellipticine,Isoellipticine,And 7-Carbethoxyisoellipticine
    标题:Preparation Of Polyfunctional Aryl Azides From Aryl Triazenes. A New Synthesis Of Ellipticine,9-Methoxyellipticine,Isoellipticine,And 7-Carbethoxyisoellipticine
    摘要:[graphics]The Preparation Of Polyfunctional Aryl Azides By The Reaction Of Aryl Triazenes With Nan3 In The Presence Of Khso4 Or Bf3 Center Dot Oet2/tfa (Trifluoroacetic Acid) Has Been Described. A Variety Of Functional Groups (Halides,Esters,Ketones,Nitriles,Aldehydes,And Boronic Esters) Are Tolerated Under The Lewis Acidic Conditions. By Using This Methodology,The Potent Antitumor Agents,Ellipticine And 9-Methoxyellipticine,Have Been Synthesized. In Addition,Isoellipticine And A Related Derivative,7-Carbethoxyisoellipticine,Were Also Prepared.
    DOI:10.1021/jo070774Z

    海关参考信息

    专利信息


    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-9662347-B2
    优先权日:2010-05-11
    标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system
    发明人:LEE BONG HEE; BYUN KYUNG HEE
    权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND
    摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.

    专利号:WO-2013087821-A1
    优先权日:2011-12-15
    标题:Overproduction of jasmonates in transgenic plants
    发明人:CHAMPION ANTONY
    权利人:INST RECH DEVELOPPEMENT IRD
    摘要:La present invention relates to the use of a nucleic sequence allowing the synthesis of Gh ERF-IIa, Gh ERF-IIb or Gh ERF-IIc in a plant in order to induce, in the plant, an overproduction or accumulation of jasmonic acid and/or OPDA. The accumulation of jasmonic acid and/or OPDA confers, in particular, to the transformed plant an improved resistance to bioagressors. The nucleic sequences, transformation methods and transformed plants according to the invention may also been used for the production of pharmaceutically important secondary metabolites whose synthesis is induced by jasmonates.

    专利号:US-5419966-A
    优先权日:1991-06-10
    标 题 :Solid support for synthesis of 3'-tailed oligonucleotides
    发明人:REED MICHAEL W; MEYER JR RICH B; PETRIE CHARLES R; TABONE JOHN C
    权利人:MICROPROBE CORP
    摘要:A solid support for oligonucleotide synthesis has the structure where CPG represents a controlled pore glass matrix, the wavy line represents a carbon chain covalently linking the NH group with the controlled pore glass matrix, X is 2,2'-dimethoxytrityl or H, and R is alkyl, aryl, arylalkyl, heteroalkyl, or heteroaryl. The dimethoxytrityl group is removed from the solid support by treatment with acid, and the oligonucleotide is built, step-by-step in a conventional synthesizer after attachment of the 3' end of the first oligonucleotide unit to the hydroxyl function connected to the R group.

    专利号:US-2007172520-A1
    优先权日:2005-11-18
    标题:Immunotargeting of Nonionic Surfactant Vesicles
    发明人:VANAUKER MICHAEL; PLAAS ANNA; HOOD ELIZABETH
    权利人:UNIV SOUTH FLORIDA
    摘要:An immunoniosmes for targeted delivery of therapeutic agents to specific tissues in a host and methods of synthesis of those niosomes. An antibody molecule having specificity for a target antigen, such as a cell surface marker or other marker differentially expressed on a target cell, is covalently coupled to a functionalized membrane constituent. In a particular embodiment the functionalized membrane constituent is polyoxyethylene sorbitan monostearate functionalized with cyanuric chloride. The niosomes of this invention thus provide a composition that enhances internalization or retention of the bioactive agent of the niosome into the cytoplasm of the cells of the target tissue by providing a high degree of target specificity. Furthermore, the membrane vesicle enhances the life of the therapeutic agent by preventing its degradation in the extracellular environment, while exhibiting lower toxicity than can occur with some liposomes. The niosomes of the present invention are thus particularly useful as vehicles for the delivery of therapeutics to specific target cells.

    专利号:US-2023288116-A1
    优先权日:2022-03-14
    标 题:Large scale synthesis of pharmaceutical and biologic formulations using thin film freezing
    发明人:OWENS III DONALD E; KOLENG JR JOHN J
    权利人:TFF PHARMACEUTICALS INC
    摘要:The invention encompasses methods for the large-scale (preferably under cGMP or cGLP standards) preparation of micron-sized or submicron-sized particles including pharmaceutical or biologic active agents. The systems and methods include a cryogenic cooling system including a novel shroud that enhances the cooling effects thereby reducing product loss and increasing product yields.

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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: Lu H, Liu M, Lu W, Wang C, Wang G, Dong W, Wang X, Chen H, Tan C. Repurposing Ellipticine Hydrochloride to Combat Colistin-Resistant Extraintestinal Pathogenic E. coli (ExPEC). Front Microbiol. 2020 May 25;11:806. doi: 10.3389/fmicb.2020.00806.
    2: Costa de Oliveira R, Soares Pontes G, Kostyuk A, Coutinho Camargo GB, Dhyani A, Shvydenko T, Shvydenko K, Grafov A. Anticancer and Immunomodulatory Activities of a Novel Water-Soluble Derivative of Ellipticine. Molecules. 2020 May 1;25(9):2130. doi: 10.3390/molecules25092130.
    3: Li X, Ye C, Mulati M, Sun L, Qian F. Ellipticine blocks synergistic effects of IL-17A and TNF-α in epithelial cells and alleviates severe acute pancreatitis-associated acute lung injury. Biochem Pharmacol. 2020 Jul;177:113992. doi: 10.1016/j.bcp.2020.113992. Epub 2020 Apr 23. 146(7):1671-1676. doi: 10.1007/s00432-020-03213-x. Epub 2020 Apr 24. 25(1):24. doi: 10.3390/molecules25010024.

    合成参考文献


    参考文献:10.2478/v10102-011-0017-7
    摘要:Stiborová M, Poljaková J, Martínková E, Bořek-Dohalská L, Eckschlager T, Kizek R, Frei E. Ellipticine cytotoxicity to cancer cell lines - a comparative study. Interdiscip Toxicol. 2011 Jun;4(2):98–105.
    参考文献:10.1007/s12672-011-0065-7
    摘要:Neubauer NL, Ward EC, Patel P, Lu Z, Lee I, Blok LJ, Hanifi-Moghaddam P, Schink J, Kim JJ. Progesterone Receptor-B Induction of BIRC3 Protects Endometrial Cancer Cells from AP1-59-Mediated Apoptosis. Discover Oncology. 2011 Feb 02;2(3):170–81. doi: 10.1007/s12672-011-0065-7.
    参考文献:10.1007/s11033-011-1164-9
    摘要:Kashanian S, Khodaei MM, Pakravan P, Adibi H. Molecular aspects on the interaction of isatin-3-isonicotinylhydrazone to deoxyribonucleic acid: model for intercalative drug-DNA binding. Molecular Biology Reports. 2011 Jul 21;39(4):3853–61. doi: 10.1007/s11033-011-1164-9.
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