[RuCl(μ-Cl)(4-formylphenoxyacetyl-η6-benzylamide)]2 | 959143-30-7

• 英文名称: [RuCl(μ-Cl)(4-formylphenoxyacetyl-η6-benzylamide)]2
• CAS: 959143-30-7
• 化学式: C₃₂H₃₀Cl₄N₂O₆Ru₂
• 分子量: 882.552
• InChiKey: HXSOWNAYJUZTDW-UHFFFAOYSA-J

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
  None
• 可旋转键数：
  None
• 环数：
  None
• sp3杂化的碳原子比例：
  None
• 拓扑面积：
  None
• 氢给体数：
  None
• 氢受体数：
  None

反应信息

• 作为反应物：
  描述：

  [RuCl(μ-Cl)(4-formylphenoxyacetyl-η6-benzylamide)]2 、 1,3,5-三氮杂-7-磷杂金刚烷 以 N,N-二甲基甲酰胺 为溶剂， 生成 [RuCl2(C6H6CH2NHCOCH2OC6H4COH)(1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane)]
  参考文献：
  名称：

  将有机金属钌-芳烃抗癌化合物束缚于重组人血清白蛋白的策略。

  摘要：

  为了利用大分子进行药物靶向和递送，开发了将有机金属钌-芳烃药物束缚到载体蛋白分子的策略。该方法涉及能够通过fragment键形成与修饰的载体蛋白上的接头分子缀合的药物片段的设计。描述了使用重组人血清白蛋白的概念验证。

  DOI：

  10.1021/ic701474m
• 作为产物：
  描述：

  水合三氯化钌 、 N-benzyl-2-(4-formylphenoxy)acetamide 以 乙醇 为溶剂， 生成 [RuCl(μ-Cl)(4-formylphenoxyacetyl-η6-benzylamide)]2
  参考文献：
  名称：

  将有机金属钌-芳烃抗癌化合物束缚于重组人血清白蛋白的策略。

  摘要：

  为了利用大分子进行药物靶向和递送，开发了将有机金属钌-芳烃药物束缚到载体蛋白分子的策略。该方法涉及能够通过fragment键形成与修饰的载体蛋白上的接头分子缀合的药物片段的设计。描述了使用重组人血清白蛋白的概念验证。

  DOI：

  10.1021/ic701474m

文献信息

• Conjugation of Organoruthenium(II) 3-(1<i>H</i>-Benzimidazol-2-yl)pyrazolo[3,4-<i>b</i>]pyridines and Indolo[3,2-<i>d</i>]benzazepines to Recombinant Human Serum Albumin: a Strategy To Enhance Cytotoxicity in Cancer Cells
  作者：Iryna N. Stepanenko、Angela Casini、Fabio Edafe、Maria S. Novak、Vladimir B. Arion、Paul J. Dyson、Michael A. Jakupec、Bernhard K. Keppler

  DOI：10.1021/ic201801e

  日期：2011.12.19

  Following our strategy of coupling cyclin-dependent kinase (Cdk) inhibitors with organometallic moieties to improve their physicochemical properties and bioavailability, five organoruthenium complexes (1c-5c) of the general formula [RuCl(eta(6)-arene)(L)]Cl have been synthesized in which the arene is 4-formylphenoxyacetyl-eta(6)-benzylamide and L is a Cdk inhibitor [3-(1H-benzimidazol-2-yl)-1H-pyrazolo[3,4-b]pyridines (L1-L3) and indolo[3,2-d]benzazepines (L4 and L5)]. All of the compounds were characterized by spectroscopic and analytical methods. Upon prolonged standing (2-3 months) at room temperature, the dimethyl sulfoxide (DMSO) solutions of 1c and 2c-(HCl) afforded residues, which after recrystallization from EtOH and EtOH/H2O, respectively, were shown by X-ray diffraction to be cis,cis-[(RuCl2)-Cl-II(DMSO)(2)(L1)]center dot H2O and mer-[(RuCl)-Cl-II(DMSO)(3)(L2-H)]center dot H2O. Compound 5c, with a coordinated amidine unit, undergoes E/Z isomerization in solution. The antiproliferative activities and effects on the cell cycle of the new compounds were evaluated. Complexes 1c-5c are moderately cytotoxic to cancer cells (CH1, SW480, A549, A2780, and A2780cisR cell lines). Therefore, in order to improve their antiproliferative effects, as well as their drug targeting and delivery to cancer cells, 1c-5c were conjugated to recombinant human serum albumin, potentially exploiting the so-called "enhanced permeability and retention" effect that results in the accumulation of macromolecules in tumors. Notably, a marked increase in cytotoxicity of the albumin conjugates was observed in all cases.