(E)-3-(2,3,4,5-Tetrabromophenyl)acrylic acid

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: (E)-3-(2,3,4,5-Tetrabromophenyl)acrylic acid
• 英文别名: (E)-3-(2,3,4,5-tetrabromophenyl)prop-2-enoic acid
• 化学式: C₉H₄Br₄O₂
• 分子量: 463.74
• InChiKey: SVJQCVOKYJWUBC-OWOJBTEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] 3 -CYANO- 5 -ARYLAMINO-7 -CYCLOALKYLAMINOPYRROLO [1, 5 -A] PYRIMIDINE DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS<br/>[FR] DÉRIVÉS DE PYRIMIDINE 3-CYANO-5-ARYLAMINO -7-CYCLOALKYLAMINOPYRROLO [1, 5-A] ET LEURS UTILISATIONS COMME AGENTS ANTITUMORAUX
  申请人：ASTRAZENECA AB

  公开号：WO2013144532A1

  公开（公告）日：2013-10-03

  The invention relates to chemical compounds of Formula (I): or a salt thereof. In some embodiments, the invention relates to inhibitors of CK2. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and treatment of CK2-related conditions and diseases, e.g., cancer.

  该发明涉及化合物的化学结构式(I)：或其盐。在某些实施例中，该发明涉及CK2的抑制剂。在更进一步的实施例中，该发明涉及包括本文披露的化合物的药物组合物及其在预防和治疗与CK2相关的疾病和疾病，例如癌症中的应用。
• NUCLEOTIDE TRIPHOSPHATE WITH AN ELECTROACTIVE LABEL CONJUGATED TO THE GAMMA PHOSPHATE
  申请人：Kraatz Heinz-Bernhard

  公开号：US20110218114A1

  公开（公告）日：2011-09-08

  A nucleotide triphosphate (NTP) participates in a phosphorylation reaction, wherein a phosphate group is transferred from the NTP to a substrate by a kinase. Provision in a kinase reaction of a NTP whose gamma phosphate is conjugated to an electroactive label results in the transfer of the gamma phosphate-electroactive label conjugate from the NTP to the substrate. The electroactive label is an organic moiety such as a quinone or a nitroheterocycle, or is a metallocene such as a ferrocene or a cobaltocene. Upon transfer of the gamma phosphate-electroactive label conjugate to an electrode-bound substrate by a kinase, the phosphorylation event is detected electrochemically by cyclic voltammetry. Phosphorylation can also be detected by mass spectrometry of a substrate carrying the electroactive label-conjugated gamma phosphate. NTP comprising the gamma phosphate-electroactive label conjugate is used in methods of detecting the presence of a kinase in a sample, screening candidate compounds that modulate kinase activity, and in methods of diagnosing a disease associated with a kinase.

  核苷酸三磷酸（NTP）参与磷酸化反应，其中通过激酶，将磷酸基从NTP转移至底物。在激酶反应中，提供一个将伽马磷酸酯化为电活性标记的NTP，结果将伽马磷酸酯-电活性标记共轭物从NTP转移至底物。电活性标记是一种有机基团，例如醌或硝基杂环，或是一种金属茂基，例如二茂铁或二茂钴。当伽马磷酸酯-电活性标记共轭物通过激酶转移至电极结合的底物时，通过循环伏安法可以电化学地检测到磷酸化事件。磷酸化还可以通过携带电活性标记共轭伽马磷酸酯的底物的质谱分析来检测。含有伽马磷酸酯-电活性标记共轭物的NTP用于检测样品中激酶的存在，筛选调节激酶活性的候选化合物，并用于诊断与激酶相关的疾病的方法。
• Methods and pharmaceutical compositions for treating microbiome dysregulations associated with circadian clock disruption
  申请人：INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE)

  公开号：US11364219B2

  公开（公告）日：2022-06-21

  The present invention relates to the treatment of microbiome dysregulations. Said dysregulations may subsequently contribute to the development of several chronic diseases. Thus characterization of new post-biotic compounds inducing beneficial changes on host-microbiota interactions may be highly desirable. The inventors showed that Nlrp6 diurnally coordinates cyclical adaptation of the gut microbiota diversity to epithelial plasticity in response to a treatment with a Csnk2 inhibitor. The invention therefore relates to an inhibitor of Csnk2, for use in the treatment of microbiome dysregulations notably associated with circadian clock disruption. Said inhibitor may be selected among chemically synthesized or natural selective Csnk2 inhibitors such as flavones.

  本发明涉及微生物组失调的治疗。这些失调可能会导致多种慢性疾病的发生。因此，对能诱导宿主-微生物群相互作用发生有益变化的新生物后化合物进行表征可能是非常可取的。本发明者的研究表明，Nlrp6 在使用 Csnk2 抑制剂治疗的情况下，会周期性地协调肠道微生物群多样性对上皮可塑性的适应。因此，本发明涉及一种 Csnk2 抑制剂，用于治疗主要与昼夜节律紊乱有关的微生物组失调。所述抑制剂可选择化学合成或天然选择性 Csnk2 抑制剂，如黄酮类。
• METHODS RELATED TO CASEIN KINASE II (CK2) INHIBITORS AND THE USE OF PURINOSOME-DISRUPTING CK2 INHIBITORS FOR ANTI-CANCER THERAPY AGENTS
  申请人：Corning Incorporated

  公开号：EP2537027A1

  公开（公告）日：2012-12-26
• VERWENDUNG VON DIBENZOFURANONDERIVATEN ZUR INHIBIERUNG VON KINASEN
  申请人：Jose, Joachim

  公开号：EP2585059A1

  公开（公告）日：2013-05-01