CAS: 174545-76-7; Eleutherobin

该化合物是海洋软珊瑚埃瑟瑟罗比亚的天然产物,以其潜在的药用特性而著称,特别是在癌症研究中;它被归类为二苯基,这是一种由四等离子细胞组成的二苯胺,其结构复杂,有助于其生物活动; 乙醚宾展示了各种癌症细胞线的细胞毒性效应,使其具有作为抗癌剂的潜力; 其行动机制被认为涉及微囊动力的破坏,类似于在化疗中常用的毒气. 此外,乙氧乙酸在调控免疫反应方面表现出希望,并研究过其抗炎特性,然而,由于其结构复杂以及与其提取和合成有关的挑战,需要进一步研究,以充分理解其药理学潜力并开发可行的治疗应用.与许多自然化合物一样,对乙氏素本的特性的探索仍然是医药化学和药理研究的一个令人振奋的领域.

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      专利信息


      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.

      专利号:US-6172205-B1
      优先权日:1997-12-11
      标题 :Synthetic process toward total synthesis of eleutherobin and its analogues and uses thereof
      发明人:DANISHEFSKY SAMUEL J; CHEN XIAO-TAO; GUTTERIDGE CLARE E; BHATTACHARYA SAMIT K; ZHOU BISHAN
      权利人:TRUSTEES OF COLUMBIA IN THE CI
      摘要:This invention provides a process for the preparation of a Eleutherobin derivative of the formula: n wherein R 1 is a hydrogen, ester, nitrile or C 2 H 4 —R wherein R 4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R 2 is a linear or branched alkyl moiety, R 3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R 4 is a hydrogen or CH 2 ,position C 2 and C 3 is cis or trans,position C 8 is α or β and a compound is produced having the structures: n Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.

      专利号:US-2017283878-A1
      优先权日:2015-12-11
      标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
      发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
      权利人:ACADEMIA SINICA
      摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

      专利号:US-2024173256-A1
      优先权日:2022-11-29
      标 题:Hdl mimicking targeted drug delivery system for the treatment of solid tumors
      发明人:SABNIS NIRUPAMA; LACKO ANDRAS; FUDALA RAFAL
      权利人:UNIV OF NORTH TEXAS HEALTH SCIENCE CENTER
      摘要:The present disclosure is directed to an SR-B1-targeting nanomicelle and compositions, methods of synthesis and methods of use thereof. The nanomicelle may be an HDL-mimetic drug delivery system and may be cross-linked with DSS. The composition may contain a therapeutic agent with the ability to treat cancers, especially sarcomas.

      专利号:US-8759632-B2
      优先权日:2005-07-05
      标 题 :Polynucleotides encoding isoprenoid modifying enzymes and methods of use thereof
      发明人:RO DAE-KYUN; NEWMAN KARYN; PARADISE ERIC M; KEASLING JAY D; OUELLET MARIO; EACHUS RACHEL; HO KIMBERLY; HAM TIMOTHY
      权利人:RO DAE-KYUN; NEWMAN KARYN; PARADISE ERIC M; KEASLING JAY D; OUELLET MARIO; EACHUS RACHEL; HO KIMBERLY; HAM TIMOTHY; UNIV CALIFORNIA
      摘要:The present invention provides isolated nucleic acids comprising nucleotide sequences encoding isoprenoid modifying enzymes, as well as recombinant vectors comprising the nucleic acids. The present invention further provides genetically modified host cells comprising a subject nucleic acid or recombinant vector. The present invention further provides a transgenic plant comprising a subject nucleic acid. The present invention further provides methods of producing an isoprenoid compound, the method generally involving culturing a subject genetically modified host cell under conditions that permit synthesis of an isoprenoid compound modifying enzyme encoded by a subject nucleic acid.

      专利号:US-2016318862-A1
      优先权日:2013-09-25
      标 题:Synthesis of delta 12-pgj3 and related compounds
      发明人:NICOLAOU KYRIACOS C; HERETSCH PHILIPP; HALE CHRISTOPHER R H; EL GHZAOUI ABDELLATIF EL MARROUNI; PULUKURI KIRAN KUMAR; YU RUOCHENG; GROVE CHARLES
      权利人:UNIV RICE WILLIAM M
      摘要:In one aspect, the present invention provides novel derivatives of Δ 12 -PGJ 3 and modular synthetic pathways to obtaining Δ 12 -PGJ 3 and derivatives thereof. In some aspects, the present derivatives of Δ 12 -PGJ 3 are useful as chemotherapeutic agents. The present disclosure also describes compositions of these derivatives as well as methods of use of the derivatives thereof.

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      主要参考文献


      1: Long BH, Carboni JM, Wasserman AJ, Cornell LA, Casazza AM, Jensen PR, Lindel T, Fenical W, Fairchild CR. Eleutherobin, a novel cytotoxic agent that induces tubulin polymerization, is similar to paclitaxel (Taxol). Cancer Res. 1998 Mar 15;58(6):1111-5. 17(10):2792-2797. doi: 10.1039/c8ob02915f. 18(6):664-669. doi: 10.1038/s41589-022-01026-2. Epub 2022 May 23.
      4: Berrué F, McCulloch MW, Kerr RG. Marine diterpene glycosides. Bioorg Med Chem. 2011 Nov 15;19(22):6702-19. doi: 10.1016/j.bmc.2011.06.083. Epub 2011 Jul 2.
      143:806-828. doi: 10.1016/j.ejmech.2017.11.062. Epub 2017 Nov 24. 37(6):789-792. doi: 10.1002/(SICI)1521-3773(19980403)37:6<789::AID- ANIE789>3.0.CO;2-3. 44(2):131-7. doi: 10.1007/s002800050957. 50(1):kuad027. doi: 10.1093/jimb/kuad027.

      合成参考文献


      参考文献:10.1007/978-1-61779-252-6_18
      摘要:Honore S, Braguer D. Investigating microtubule dynamic instability using microtubule-targeting agents. Methods Mol Biol. 2011;777():245–60. doi: 10.1007/978-1-61779-252-6_18.
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