5-glycinamido-1,10-phenanthroline | 152572-68-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 菲咯啉
• 英文名称: 5-glycinamido-1,10-phenanthroline
• 英文别名: 2-Amino-N-(1,10-phenanthrolin-5-yl)acetamide
• CAS: 152572-68-4
• 化学式: C₁₄H₁₂N₄O
• 分子量: 252.275
• InChiKey: MALYNSGWEDWRMV-UHFFFAOYSA-N

物化性质

• 沸点：
  577.0±40.0 °C(Predicted)
• 密度：
  1.394±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  80.9
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-glycinamido-1,10-phenanthroline 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 51.0h， 生成
  参考文献：
  名称：

  带有含RGD的环五肽的多价光反应性RuII-杯[4]芳烃配合物的合成和光物理研究。

  摘要：

  人们正在积极研究光敏钌基络合物的生物学应用，将其作为潜在的抗肿瘤治疗剂。这些无机复合物的一个主要问题是渗透到细胞内部以实现其功能，或者感知内部细胞环境或发挥光细胞毒性活性。亲脂性配体的使用允许相应的钌配合物在细胞内被动扩散，但限制了它们的结构和光物理性质。而且，该策略不提供任何细胞选择性。锚定在穿透细胞的肽上的复合物也面临该限制。为了提供选择性的细胞靶向，我们开发了一种多价体系，该体系由光反应性钌（II）配合物束缚到带有多个含RGD的环五肽的杯[4]芳烃平台上。该Ru（II）-杯芳烃共轭物的广泛的光物理和光化学表征以及在鸟苷一磷酸鸟嘌呤存在下对其光反应性的研究已经实现。结果表明，钌络合物一旦通过多价平台结合到靶向癌细胞中，便应能够有效地发挥其光诱导的细胞毒活性。

  DOI：

  10.3762/bjoc.14.150
• 作为产物：
  描述：

  5-((N-(tert-butoxycarbonyl)glycyl)amino)-1,10-phenanthroline 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 5-glycinamido-1,10-phenanthroline
  参考文献：
  名称：

  Luminescent molecules towards precise cellular event regulation

  摘要：

  开发了一种对近红外(NIR)刺激做出反应的独特的镧系络合物，用于远程调节细胞事件。

  DOI：

  10.1039/d0cc01923b

文献信息

• Method of treatment of a BCL-2 disorder using BCL-2 antisense oligomers
  申请人：GENTA INCORPORATED

  公开号：EP2135623A1

  公开（公告）日：2009-12-23

  The present invention is directed to the use of bcl-2 antisense oligomers to treat and prevent bcl-2 related disorders. These disorders include cancers, tumors, carcinomas and cell-proliferative related disorders. In one embodiment of the invention, a bel-2 antisense oligomer is administered at high doses. The present invention is also directed to a method of preventing or treating a bcl-2 related disorder, in particular cancer, comprising administering a bcl-2 antisense oligomer for short periods of time. The present invention is further drawn to the use of bcl-2 antisense oligomers to increase the sensitivity of a subject to cancer therapeutics. The present invention also relates to pharmaceutical compositions comprising one or more bcl-2 antisense oligomers, which may comprise one or more cancer therapeutic agents.

  本发明涉及使用 bcl-2 反义寡聚体治疗和预防 bcl-2 相关疾病。这些疾病包括癌症、肿瘤、癌和细胞增殖相关疾病。在本发明的一个实施方案中，bel-2 反义寡聚体以高剂量给药。本发明还涉及一种预防或治疗 bcl-2 相关疾病，特别是癌症的方法，包括短期施用 bcl-2 反义寡聚体。本发明进一步涉及使用 bcl-2 反义寡聚体来提高受试者对癌症疗法的敏感性。本发明还涉及包含一种或多种bcl-2反义寡聚体的药物组合物，其中可包含一种或多种癌症治疗剂。
• Methods and compositions for treating a cell-proliferative disorder using CRE decoy oligomers, BCL-2 antisense oligomers, and hybrid oligomers thereof
  申请人：——

  公开号：US20030176376A1

  公开（公告）日：2003-09-18

  The present invention is directed to hybrid oligomers comprising a cyclic AMP response element (CRE) sequence and a sequence that hybridizes to a bcl-2 pre-mRNA or mRNA, and pharmaceutical compositions comprising such hybrids. The present invention is also directed to the use of CRE decoy oligomers, comprising a CRE consensus sequence, and bcl-2 antisense oligomers in combination therapies, and the use of bcl-2/CRE hybrid oligomers, to treat or prevent cell-proliferative related disorders, including hyperplasias, cancers, tumors and carcinomas. In one embodiment, the invention relates to therapeutic protocols comprising the administration of a CRE decoy oligomer and a bcl-2 antisense oligomer for the treatment of cell-proliferative related disorders. In another embodiment, the invention relates to therapeutic protocols comprising the administration of a bcl-2 antisense/CRE decoy (bcl-2/CRE) hybrid oligomer for the treatment of cell-proliferative related disorders.

  本发明涉及包含环磷酸腺苷反应元件（CRE）序列和与bcl-2前mRNA或mRNA杂交的序列的杂交寡聚物，以及包含这种杂交物的药物组合物。本发明还涉及包含 CRE 共识序列的 CRE 诱饵低聚物和 bcl-2 反义低聚物在联合疗法中的使用，以及 bcl-2/CRE 杂交低聚物在治疗或预防细胞增殖相关疾病（包括增生、癌症、肿瘤和癌）中的使用。在一个实施方案中，本发明涉及治疗方案，包括施用 CRE 诱饵寡聚体和 bcl-2 反义寡聚体来治疗细胞增殖相关疾病。在另一个实施方案中，本发明涉及用于治疗细胞增殖相关疾病的治疗方案，包括施用一种bcl-2反义/CRE诱饵（bcl-2/CRE）混合寡聚体。
• Methods of treatment of a bcl-2 disorder using bcl-2 antisense oligomers
  申请人：——

  公开号：US20040147473A1

  公开（公告）日：2004-07-29

  The present invention is directed to the use of bcl-2 antisense oligomers to treat and prevent bcl-2 related disorders. These disorders include cancers, tumors, carcinomas and cell-proliferative related disorders. In one embodiment of the invention, a bcl-2 antisense oligomer is administered at high doses. The present invention is also directed to a method of preventing or treating a bcl-2 related disorder, in particular cancer, comprising administering a bcl-2 antisense oligomer for short periods of time. The present invention is further drawn to the use of bcl-2 antisense oligomers to increase the sensitivity of a subject to cancer therapeutics. The present invention also relates to pharmaceutical compositions comprising one or more bcl-2 antisense oligomers, which may comprise one or more cancer therapeutic agents.

  本发明涉及使用 bcl-2 反义寡聚体治疗和预防 bcl-2 相关疾病。这些疾病包括癌症、肿瘤、癌和细胞增殖相关疾病。在本发明的一个实施方案中，bcl-2 反义寡聚体以高剂量给药。本发明还涉及一种预防或治疗 bcl-2 相关疾病，特别是癌症的方法，包括短期施用 bcl-2 反义寡聚体。本发明进一步涉及使用 bcl-2 反义寡聚体来提高受试者对癌症疗法的敏感性。本发明还涉及包含一种或多种bcl-2反义寡聚体的药物组合物，其中可包含一种或多种癌症治疗剂。
• Breast cancer-associated genes and uses thereof
  申请人：Seth Arun

  公开号：US20050065333A1

  公开（公告）日：2005-03-24

  The present invention relates to seven isolated breast cancer-associated (BCA) polynucleotides, polypeptides, and variants thereof. The invention also relates to BCA antagonists. The invention also encompasses pharmaceutical compositions comprising BCA polynucleotides, BCA polypeptides, or BCA antagonists. The invention also contemplates methods for preventing or treating cancer, particularly breast cancer, comprising administering to a patient in need of such treatment a composition comprising a BCA polynucleotide, polypeptide, antagonist, or variant thereof. The invention also relates to methods for diagnosing, staging or determining a prognosis of a BCA-related disorder.

  本发明涉及七种分离的乳腺癌相关（BCA）多核苷酸、多肽及其变体。 本发明还涉及 BCA 拮抗剂。 本发明还包括包含 BCA 多核苷酸、BCA 多肽或 BCA 拮抗剂的药物组合物。 本发明还考虑了预防或治疗癌症，特别是乳腺癌的方法，包括向需要这种治疗的患者施用包含BCA多核苷酸、多肽、拮抗剂或其变体的组合物。 本发明还涉及诊断、分期或确定BCA相关疾病的预后的方法。
• Synthesis of an oxyamino-containing phenanthroline derivative for the efficient preparation of phenanthroline oligonucleotide oxime conjugates
  作者：Stéphanie Deroo、Eric Defrancq、Cécile Moucheron、Andrée Kirsch-De Mesmaeker、Pascal Dumy

  DOI：10.1016/j.tetlet.2003.09.128

  日期：2003.11

  A phenanthroline derivative bearing an oxyamino linker was efficiently prepared from commercial 5-nitro-1,10-phenanthroline. The subsequent reaction with an oligonucleotide containing an aldehyde either at the 5' end or the 3' end afforded, in good yield, the phenanthroline-oligonucleotide conjugates through oxime bond formation. (C) 2003 Elsevier Ltd. All rights reserved.