methyl 4-(2-aminoacetamido)-3-methoxybenzoate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: methyl 4-(2-aminoacetamido)-3-methoxybenzoate
• 英文别名: 4-(2-Amino-acetylamino)-3-methoxy-benzoic acid methyl ester；methyl 4-[(2-aminoacetyl)amino]-3-methoxybenzoate
• 化学式: C₁₁H₁₄N₂O₄
• 分子量: 238.243
• InChiKey: JYWBAYPGOTZIRT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  90.6
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  methyl 4-(2-aminoacetamido)-3-methoxybenzoate 在 copper diacetate 、 magnesium sulfate 、 (R)-2,2'-bis(diphenylphosphanyl)-1,1'-binaphthyl 、 三乙胺 作用下， 以 2-甲基四氢呋喃 、 二氯甲烷 为溶剂， 反应 23.0h， 生成 Idasanutlin（4-（（2R,3S,4R,5S）-3-（3-氯-2-氟苯基）-4-（4-氯-2-氟苯基）-4-氰基-5-新戊基吡咯烷-2-甲酰胺）-3-甲氧基苯甲酸;）
  参考文献：
  名称：

  [EN] PHOTORESPONSIVE NUTLIN DERIVATIVES AND USES THEREOF
  [FR] DÉRIVÉS DE NUTLINE PHOTOSENSIBLES ET LEURS UTILISATIONS

  摘要：

  这项发明涉及医学和药物化学领域，更具体地涉及设计、制造和使用可以通过外部刺激激活的抗癌药物，该外部刺激可以以时空方式应用。本文提供了具有该化学结构或其药用可接受盐的化合物。

  公开号：

  WO2020071911A1
• 作为产物：
  描述：

  3-甲氧基-4-氨基苯甲酸甲酯 在 ammonium hydroxide 、 三乙胺 作用下， 以 乙醇 、 二氯甲烷 为溶剂， 生成 methyl 4-(2-aminoacetamido)-3-methoxybenzoate
  参考文献：
  名称：

  [EN] PHOTORESPONSIVE NUTLIN DERIVATIVES AND USES THEREOF
  [FR] DÉRIVÉS DE NUTLINE PHOTOSENSIBLES ET LEURS UTILISATIONS

  摘要：

  这项发明涉及医学和药物化学领域，更具体地涉及设计、制造和使用可以通过外部刺激激活的抗癌药物，该外部刺激可以以时空方式应用。本文提供了具有该化学结构或其药用可接受盐的化合物。

  公开号：

  WO2020071911A1

文献信息

• SPIROPYRROLIDINES AS MDM2 INHIBITORS
  申请人：HUDSON BIOPHARMA INC.

  公开号：US20150322076A1

  公开（公告）日：2015-11-12

  Described are spiropyrrolidines (I) useful as inhibitors of MDM2/p53 interactions and provides useful agents for the treatment of diseases like cancer and retinal macular degeneration diseases. The invented compounds herein have the general Further described are pharmaceutical compositions that comprise one or more compounds of the invention, a pharmaceutically acceptable salt or pro-drug and/or a pharmaceutically acceptable carrier or excipient.

  描述了作为MDM2/p53相互作用抑制剂的螺环吡咯烷(I)，并提供了用于治疗癌症和视网膜黄斑变性等疾病的有用药剂。本发明的化合物具有一般性。进一步描述了包括本发明的一个或多个化合物、药学上可接受的盐或前药以及药学上可接受的载体或赋形剂的药物组合物。
• Spirocyclic indolone polyethylene glycol carbonate compound, composition, preparation method and use thereof
  申请人：Xiao Fei

  公开号：US10471154B2

  公开（公告）日：2019-11-12

  The present invention relates to a spirocyclic indolone polyethylene glycol carbonate compound, a composition thereof, a preparation method therefor, and a use thereof as an anticancer drug due to the antitumor activity thereof. The structural formula of the spirocyclic indolone polyethylene glycol carbonate compound is shown below. The compound has excellent tumor inhibitory activity, water solubility, low toxicity, and can be used for intravenous injection.

  本发明涉及一种螺环吲哚酮聚乙二醇碳酸酯化合物、其组合物、其制备方法以及由于其抗肿瘤活性而作为抗癌药物的用途。螺环吲哚酮聚乙二醇碳酸酯化合物的结构式如下所示。该化合物具有优异的肿瘤抑制活性、水溶性、低毒性，可用于静脉注射。
• Photoactivation of MDM2 Inhibitors: Controlling Protein–Protein Interaction with Light
  作者：Mickel J. Hansen、Femke M. Feringa、Piermichele Kobauri、Wiktor Szymanski、René H. Medema、Ben L. Feringa

  DOI：10.1021/jacs.8b04870

  日期：2018.10.17

  Selectivity remains a major challenge in anticancer therapy, which potentially can be overcome by local activation of a cytotoxic drug. Such triggered activation can be obtained through modification of a drug with a photoremovable protecting group (PPG), and subsequent irradiation in the chosen place and time. Herein, the design, synthesis and biological evaluation is described of a photoactivatable MDM2 inhibitor, PPG-idasanutlin, which exerts no functional effect on cellular outgrowth, but allows for the selective, noninvasive activation of antitumor properties upon irradiation visible light, demonstrating activation with micrometer, single cell precision. The generality of this method has been demonstrated by growth inhibition of multiple cancer cell lines showing p53 stabilization and subsequent growth inhibition effects upon irradiation. Light activation to regulate protein-protein interactions between MDM2 and p53 offers exciting opportunities to control a multitude of biological processes and has the potential to circumvent common selectivity issues in antitumor drug development.
• PHOTORESPONSIVE NUTLIN DERIVATIVES AND USES THEREOF
  申请人：RIJKSUNIVERSITEIT GRONINGEN

  公开号：EP3860654A1

  公开（公告）日：2021-08-11
• SPIROCYCLIC INDOLONE POLYETHYLENE GLYCOL CARBONATE COMPOUND, COMPOSITION, PREPARATION METHOD AND USE THEREOF
  申请人：Xiao Fei

  公开号：US20190209700A1

  公开（公告）日：2019-07-11

  The present invention relates to a spirocyclic indolone polyethylene glycol carbonate compound, a composition thereof, a preparation method therefor, and a use thereof as an anticancer drug due to the antitumor activity thereof The structural formula of the spirocyclic indolone polyethylene glycol carbonate compound is shown below. The compound has excellent tumor inhibitory activity, water solubility, low toxicity, and can be used for intravenous injection.