suberamic acid | 73427-53-9

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: suberamic acid
• 英文别名: 8-Amino-8-oxooctanoic acid
• CAS: 73427-53-9
• 化学式: C₈H₁₅NO₃
• 分子量: 173.212
• InChiKey: NZRWECQCBREPPG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  12
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  80.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  suberamic acid 在 4-二甲氨基吡啶 、 苯甲醚 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三氟乙酸 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 0.25h， 生成 phorbol 12-O-suberamide-13-acetate
  参考文献：
  名称：

  Protein Kinase C Translocation by Modified Phorbol Esters with Functionalized Lipophilic Regions

  摘要：

  Several novel phorbol esters were prepared with polar functional groups terminating their C12 and/or C13 acyl chains. Designed to be inhibitory protein kinase C (PKC) ligands, these phorbol analogues contain various polar functional groups (amide, ester, carboxylic acid, or quaternary ammonium salt) to prevent membrane insertion of the PKC-phorbol ester complex. All phorbol derivatives were synthesized with use of diterpene starting materials obtained from croton oil, the seed oil of Croton tiglium. The ability of these derivatives to recruit PKC to the lipid bilayer-a usual requirement for enzyme activation-was determined by using a sucrose-loaded vesicle assay. Phorbol 12-octanoate-13-acetate derivatives translocate PKC-betaII to increasing degrees as the functionality on the C12 ester becomes more hydrophobic. Likewise, PKC translocation by carboxylic acid-containing phorbol esters was dependent upon length and saturation of the hydrocarbon tether. The most promising PKC inhibitors had short carboxylic acids capping their C12 and C13 acyl chains, since these compounds did not recruit PKC to any appreciable extent.

  DOI：

  10.1021/jo030029w
• 作为产物：
  描述：

  辛二酸单甲酯 在 氨 、 水 作用下， 生成 suberamic acid
  参考文献：
  名称：

  Anchel, Archives of Biochemistry, 1958, vol. 78, p. 100,105

  摘要：

  DOI：

文献信息

• [EN] DERIVATIVES OF AMANITA TOXINS AND THEIR CONJUGATION TO A CELL BINDING MOLECULE<br/>[FR] DÉRIVÉS DE TOXINES D'AMANITES ET LEUR CONJUGAISON À UNE MOLÉCULE DE LIAISON CELLULAIRE
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2017046658A1

  公开（公告）日：2017-03-23

  Derivatives of Amernita toxins of Formula (I), wherein, formula (a) R 1, R 2, R 3, R 4, R 5, R 6, R 7, R 8, R 9, R 10, X, L, m, n and Q are defined herein. The preparation of the derivatives. The therapeutic use of the derivatives in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.

  Amernita毒素的衍生物的化学式（I），其中，化学式（a）中的R 1、R 2、R 3、R 4、R 5、R 6、R 7、R 8、R 9、R 10、X、L、m、n和Q在此处被定义。这些衍生物的制备。这些衍生物在靶向治疗癌症、自身免疫性疾病和传染病中的治疗用途。
• [EN] NOVEL CYTOTOXIC AGENTS FOR CONJUGATION OF DRUGS TO CELL BINDING MOLECULE<br/>[FR] NOUVEAUX AGENTS CYTOTOXIQUES POUR LA CONJUGAISON DE MÉDICAMENTS AVEC LA MOLÉCULE DE LIAISON CELLULAIRE
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2015028850A1

  公开（公告）日：2015-03-05

  Provided are cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.

  提供了细胞毒性药物，吡咯并[2,1-c][1,4]苯二氮杂环己烷（PBD）衍生物，它们与细胞结合剂的结合物，以及在靶向治疗癌症、自身免疫性疾病和传染病中的制备和治疗用途。
• Heterolytic (2 e) vs Homolytic (1 e) Oxidation Reactivity: N−H versus C−H Switch in the Oxidation of Lactams by Dioxirans
  作者：Cosimo Annese、Lucia D'Accolti、Caterina Fusco、Giulia Licini、Cristiano Zonta

  DOI：10.1002/chem.201604507

  日期：2017.1.5

  in the oxidation of lactams moving from dimethyl dioxirane (DDO) to methyl(trifluoromethyl)dioxirane (TFDO). A physical organic chemistry study, which combines the oxidation with two other dioxiranes methyl(fluoromethyl)dioxirane, MFDO, and methyl(difluoromethyl)dioxirane, DFDO, with computational studies, points to a diverse ability of the dioxiranes to either stabilize the homo or the heterolytic

  二恶英是强大的氧化剂，可通过两种不同的机制起作用：1）均溶（H提取和氧回弹）和2）杂溶（亲电子氧化）。迄今为止，已经报道了底物的性质决定了反应模式，而与所使用的二环氧乙烷无关。在此，我们报道了前所未有的情况，其中二环氧乙烷的性质决定了氧化化学选择性。特别是，在内酰胺从二甲基二环氧乙烷（DDO）转移到甲基（三氟甲基）二环氧乙烷（TFDO）的内酰胺氧化中观察到了从CH到NH的转换。一项物理有机化学研究，将氧化与其他两种二氧杂环戊烷甲基（氟甲基）二环氧乙烷，MFDO和甲基（二氟甲基）二环氧乙烷相结合，通过计算研究，DFDO指出二恶英类化合物具有稳定同源或杂合途径的多种能力。
• [EN] MODIFIED NUCLEOSIDES<br/>[FR] NUCLÉOSIDES MODIFIÉS
  申请人：UNIV KONSTANZ

  公开号：WO2017097973A1

  公开（公告）日：2017-06-15

  The present invention relates to modified nucleosides which are linked to cargo molecules and which can be incorporated by DNA or RNA polymerases in strand synthesis. The present invention also relates to use of such modified nucleosides as substrates for DNA or RNA polymerases. The present invention also relates to the use of such modified nucleosides in diagnosis and prognosis of diseases or disorders associated with a target sequence. The present invention also relates to methods for producing such modified nucleosides, kits comprising such nucleosides, and in vitro methods for diagnosing or predicting diseases or disorders associated with a target sequence. The present invention also relates to modified nucleosides for use in diagnosing, predicting or treating diseases or disorders associated with a target sequence.

  本发明涉及与载荷分子连接的修饰核苷，可以由DNA或RNA聚合酶在链合成中合并。本发明还涉及将这种修饰核苷用作DNA或RNA聚合酶的底物的用途。本发明还涉及将这种修饰核苷用于诊断和预测与靶序列相关的疾病或紊乱的用途。本发明还涉及生产这种修饰核苷的方法，包括这种核苷的试剂盒，以及用于诊断或预测与靶序列相关的疾病或紊乱的体外方法。本发明还涉及用于诊断、预测或治疗与靶序列相关的疾病或紊乱的修饰核苷。
• [EN] TYROSINE KINASE 2 (TYK2) DEGRADATION COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS DE DÉGRADATION DE LA TYROSINE KINASE 2 (TYK2) ET PROCÉDÉS D'UTILISATION
  申请人：CULLGEN SHANGHAI INC

  公开号：WO2022100710A1

  公开（公告）日：2022-05-19

  This disclosure relates to heterobifunctional compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the heterobifunctional compounds, and to methods of use the heterobifunctional compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such heterobifunctional compounds.

  本公开涉及异双官能团化合物（例如，双官能团小分子化合物），包含一种或多种异双官能团化合物的组合物，以及使用异双官能团化合物治疗需要该治疗的患者的某些疾病的方法。本公开还涉及识别这种异双官能团化合物的方法。