2-(2-(2-(2-(adamantan-1-yloxy)ethoxy)ethoxy)ethoxy)ethanamine | 938078-76-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(2-(2-(2-(adamantan-1-yloxy)ethoxy)ethoxy)ethoxy)ethanamine
• 英文别名: 2-(2-{2-[2-(adamantan-1-yloxy)ethoxy]ethoxy}ethoxy)ethanamine；2-aminoethyl triethylene glycol adamantyl ether；2-(2-(2-(2-(Adamantan-1-yloxy)ethoxy)ethoxy)ethoxy)ethanamine；2-[2-[2-[2-(1-adamantyloxy)ethoxy]ethoxy]ethoxy]ethanamine
• CAS: 938078-76-3
• 化学式: C₁₈H₃₃NO₄
• 分子量: 327.464
• InChiKey: YLELVOJCCXYTSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  23
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  62.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  碘代乙酸酐 、 2-(2-(2-(2-(adamantan-1-yloxy)ethoxy)ethoxy)ethoxy)ethanamine 在 N,N-二异丙基乙胺 作用下， 反应 1.0h， 生成 N-[2-[2-[2-[2-(1-adamantyloxy)ethoxy]ethoxy]ethoxy]ethyl]-2-iodoacetamide
  参考文献：
  名称：

  Nanometer Arrays of Functional Light Harvesting Antenna Complexes by Nanoimprint Lithography and Host−Guest Interactions

  摘要：

  We show an approach based on combination of site-directed mutagenesis, NIL and multivalent host-guest interactions for the realization of engineered ordered functional arrays of purified components of the photosynthetic system, the membrane-bound LH2 complex. In addition to micrometer-scale patterned structures, we demonstrated the use of nanometer-scale hard NIL stamps to generate functional protein arrays approaching molecular dimensions.

  DOI：

  10.1021/ja802843m
• 作为产物：
  描述：

  1-溴金刚烷 在 sodium azide 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 三乙胺 、 三苯基膦 作用下， 以 四氢呋喃 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 72.0h， 生成 2-(2-(2-(2-(adamantan-1-yloxy)ethoxy)ethoxy)ethoxy)ethanamine
  参考文献：
  名称：

  通过疏水标记小分子介导的雄激素受体降解

  摘要：

  雄激素受体（AR）依赖性转录是前列腺肿瘤细胞增殖的主要驱动因素。因此，它是多种抗肿瘤化疗药物的靶点，包括 AR 拮抗剂 MDV3100/恩杂鲁胺。最近的研究表明，单个 AR 突变 (F876L) 可将 MDV3100 的作用从拮抗剂转变为激动剂。在这里，我们描述了一类新型选择性雄激素受体降解剂（SARD）的产生，以解决这种耐药机制。含有与小分子 AR 配体连接的疏水性降解决定子的分子可诱导 AR 降解，减少 AR 靶基因的表达并抑制雄激素依赖性前列腺癌细胞系的增殖。这些结果表明，在 AR 突变对第二代 AR 拮抗剂产生耐药性的情况下，选择性 AR 降解可能是一种有效的治疗前列腺肿瘤的策略。

  DOI：

  10.1002/anie.201503720

文献信息

• [EN] COMPOUNDS USEFUL FOR PROMOTING PROTEIN DEGRADATION AND METHODS USING SAME<br/>[FR] COMPOSÉS UTILES POUR STIMULER LA DÉGRADATION DES PROTÉINES ET PROCÉDÉS UTILISANT CEUX-CI
  申请人：UNIV YALE

  公开号：WO2013170147A1

  公开（公告）日：2013-11-14

  The present invention includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In one embodiment, the invention comprises a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. The target protein contemplated within the invention comprises a posttranslational modified protein or intracellular protein. Compounds of the present invention may be used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.

  本发明包括作为目标蛋白质降解剂的化合物，其中降解与目标蛋白质的类别或其定位无关。在一种实施方式中，该发明包括一种化合物，其中蛋白质降解基团与连接剂共价结合，该化合物的ClogP等于或高于1.5。本发明中考虑的目标蛋白质包括后转录修饰蛋白质或细胞内蛋白质。本发明的化合物可用于治疗蛋白质降解是一种可行的治疗方法的疾病状态，如癌症或任何一种氧化应激疾病状态。
• Compounds Useful for Promoting Protein Degradation and Methods Using Same
  申请人：Yale University

  公开号：US20160022642A1

  公开（公告）日：2016-01-28

  The present description includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In certain embodiments, the description includes a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. The target protein contemplated within the description comprises an androgen receptor. Compounds of the present description may be used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.

  本描述包括作为目标蛋白质降解剂的化合物，其中降解与目标蛋白质的类别或其定位无关。在某些实施例中，描述包括一种化合物，其中蛋白质降解基团与连接剂共价结合，该化合物的ClogP等于或高于1.5。描述中考虑的目标蛋白质包括雄激素受体。本描述的化合物可用于治疗蛋白质降解是可行治疗方法的疾病状态，如癌症或任何一种氧化应激疾病状态。
• Targeted LipoCEST Contrast Agents for Magnetic Resonance Imaging: Alignment of Aspherical Liposomes on a Capillary Surface
  作者：Dirk Burdinski、Jeroen A. Pikkemaat、Mustafa Emrullahoglu、Francesca Costantini、Willem Verboom、Sander Langereis、Holger Grüll、Jurriaan Huskens

  DOI：10.1002/anie.200905731

  日期：2010.3.15

  Searching for orientation: The alignment of aspherical paramagnetic liposomes in a magnetic field makes them attractive contrast agents for magnetic resonance (MR) imaging. The orientation of aspherical liposomes in solution, and the orientation change upon binding to a target surface was determined by using a simple MR technique (see picture).

  寻找方向：非球形顺磁性脂质体在磁场中的排列使其成为用于磁共振（MR）成像的有吸引力的造影剂。通过使用简单的MR技术确定溶液中非球面脂质体的取向以及与目标表面结合后的取向变化（参见图片）。
• COMPOUNDS USEFUL FOR PROMOTING PROTEIN DEGRADATION AND METHODS USING SAME
  申请人：YALE UNIVERSITY

  公开号：US20150119435A1

  公开（公告）日：2015-04-30

  The present invention includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In certain embodiments, the invention comprises a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. In other embodiments, the target protein contemplated within the invention comprises a posttranslational modified protein or intracellular protein. In yet other embodiments, compounds of the present invention are used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.

  本发明涉及作为目标蛋白质降解剂的化合物，其中降解独立于目标蛋白质的类别或其定位。在某些实施例中，本发明包括一种化合物，该化合物包括与链接物共价结合的蛋白质降解基团，其中化合物的ClogP等于或高于1.5。在其他实施例中，本发明中考虑的目标蛋白质包括后翻译修饰蛋白质或细胞内蛋白质。在其他实施例中，本发明的化合物被用于治疗蛋白质降解是一种有效的治疗方法的疾病状态，例如癌症或任何形式的氧化应激疾病状态。
• Expression of Sensitized Eu³⁺ Luminescence at a Multivalent Interface
  作者：Shu-Han Hsu、M. Deniz Yilmaz、Christian Blum、Vinod Subramaniam、David N. Reinhoudt、Aldrik H. Velders、Jurriaan Huskens

  DOI：10.1021/ja904747p

  日期：2009.9.9

  Assembly of a mixture of guest-functionalized antenna and Eu3+-complexed ligand molecules in a patterned fashion onto a receptor surface provides efficient localized sensitized emission. Coordination of a carboxylate group of the antenna to the Eu3+ center and noncovalent anchoring of both components to the receptor surface appeared to be prerequisites for efficient energy transfer. A Job plot at the surface confirmed that coordination of the antenna to the Eu3+ center occurs in a 1:1 fashion. The efficiency of this intramolecular binding process is promoted by the high effective concentration of both complementary moieties at the surface. The system constitutes therefore an example supramolecular expression of a complex consisting of several different building blocks which signals its own correct formation.