1-(6-(methylamino)naphthalen-2-yl)ethanone

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-(6-(methylamino)naphthalen-2-yl)ethanone
• 英文别名: 2-acetyl-6-methylaminonaphthalene；6-acetyl-N-methyl-2-naphthylamine；2-Acetyl6-methylaminonaphthalene；1-[6-(methylamino)naphthalen-2-yl]ethanone
• 化学式: C₁₃H₁₃NO
• 分子量: 199.252
• InChiKey: IJNAHIIIQZMFNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(6-(methylamino)naphthalen-2-yl)ethanone 在 potassium carbonate 、 三乙胺 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 反应 5.0h， 生成 N-(6-acetylnaphthalen-2-yl)-2-[bis(pyridin-2-ylmethyl)amino]-N-methylacetamide
  参考文献：
  名称：

  Studies on acedan-based mononuclear zinc complexes toward selective fluorescent probes for pyrophosphate

  摘要：

  我们已经证明了带有辅助配体的单核锌(II)–二吡啶胺(DPA)配合物能够荧光区分焦磷酸与三磷酸腺苷，其选择性可与已知的快速响应双核双(ZnDPA)配合物相媲美。

  DOI：

  10.1039/c2ob26000j
• 作为产物：
  描述：

  6-溴-2-萘酚 在 sodium disulfite 、 1,3-双(二苯基膦)丙烷 、 palladium diacetate 、 三乙胺 作用下， 以 水 、 乙二醇 为溶剂， 反应 52.0h， 生成 1-(6-(methylamino)naphthalen-2-yl)ethanone
  参考文献：
  名称：

  Studies on acedan-based mononuclear zinc complexes toward selective fluorescent probes for pyrophosphate

  摘要：

  我们已经证明了带有辅助配体的单核锌(II)–二吡啶胺(DPA)配合物能够荧光区分焦磷酸与三磷酸腺苷，其选择性可与已知的快速响应双核双(ZnDPA)配合物相媲美。

  DOI：

  10.1039/c2ob26000j

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。
• Two-Photon Fluorescent Probes for Long-Term Imaging of Calcium Waves in Live Tissue
  作者：Hwan Myung Kim、Bo Ra Kim、Myoung Jin An、Jin Hee Hong、Kyoung J. Lee、Bong Rae Cho

  DOI：10.1002/chem.200701453

  日期：2008.2.27

  ene-derived two-photon fluorescent Ca2+ probes (ACa1-ACa3) are reported. They can be excited by a 780 nm laser beam, show 23-50-fold enhancement in one- and two-photon excited fluorescence in response to Ca2+, emit fourfold stronger two-photon excited fluorescence than Oregon Green 488 BAPTA-1 upon complexation with Ca2+, and can selectively detect intracellular free Ca2+ ions in live cells and living

  报告了2-乙酰基-6-（二甲基氨基）萘衍生的双光子荧光Ca2 +探针（ACa1-ACa3）。它们可以被780 nm激光束激发，响应Ca2 +，在单光子和双光子激发的荧光中显示23-50倍的增强，在与Oregon Green 488 BAPTA-1络合后发射出比俄勒冈绿色488 BAPTA-1强四倍的光子Ca2 +，可以选择性地检测活细胞和活组织中的细胞内游离Ca2 +离子，而不受其他金属离子和膜结合探针的干扰最小。此外，这些探针能够使用双光子显微镜在无光漂白伪影的情况下，在1100-4000 s的时间内监测活组织中120-170微米深度的钙波。
• Two-photon probe for real-time monitoring of intracellular magnesium ions, method for preparing the two-photon probe and method for real-time monitoring of intracellular magnesium ions using the two-photon probe
  申请人：Korea University Industry and Academy Cooperation Foundation

  公开号：US07888532B2

  公开（公告）日：2011-02-15

  A two-photon probe for real-time monitoring of intracellular magnesium ions is provided. Specifically, the two-photon probe is represented by Formula 1: wherein R is H or CH2OCOCH3. The two-photon probe is very suitable for real-time imaging of intracellular magnesium ions. The two-photon probe shows 17-fold two-photon excited fluorescence enhancement in response to Mg2+, which is 7-fold stronger than commercial probes, thus enabling staining of cells in a greatly reduced amount. In addition, the two-photon probe has a sufficiently low molecular weight to stain cells and is very suitable for monitoring Mg2+ ions present in the deep tissue. Furthermore, the two-photon probe can be effectively used for the quantitative as well as qualitative detection of intracellular magnesium ions. Further provided are a method for preparing the two-photon probe and a method for real-time monitoring of intracellular magnesium ions using the two-photon probe.

  提供一个用于实时监测细胞内镁离子的双光子探针。具体而言，所提供的双光子探针由公式1表示：其中R是H或CH2OCOCH3。该双光子探针非常适合用于实时成像细胞内镁离子。该双光子探针对Mg2+的反应显示出17倍的双光子激发荧光增强，比商业探针强7倍，因此能够在极大地减少的量中对细胞进行染色。另外，该双光子探针具有足够低的分子量以对细胞进行染色，并且非常适合监测存在于深层组织中的Mg2+离子。此外，该双光子探针可以有效地用于定性和定量检测细胞内镁离子。进一步提供了一种制备双光子探针的方法以及一种使用双光子探针实时监测细胞内镁离子的方法。
• Highly selective fluorescence imaging of zinc distribution in HeLa cells and Arabidopsis using a naphthalene-based fluorescent probe
  作者：Ji Ha Lee、Jin Hyeok Lee、Sung Ho Jung、Tae Kyung Hyun、Mingxiao Feng、Jae-Yean Kim、Jae-Hong Lee、Hoyeon Lee、Jong Seung Kim、Chulhun Kang、Ki-Young Kwon、Jong Hwa Jung

  DOI：10.1039/c5cc01364j

  日期：——

  2-(N,N-Dimethylamino)naphthalene-based probe 1 was found to exhibit a dramatic enhancement in fluorescence upon addition of Zn²⁺, but not with any other metal ions.

  2-(N,N-二甲基氨基)萘基探针1在添加Zn2+后显示出荧光显著增强，但对其他金属离子没有这种效应。