1-(3-Chlorophenyl)-3-(diethylamino)pyrrolidine-2,5-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-(3-Chlorophenyl)-3-(diethylamino)pyrrolidine-2,5-dione
• 化学式: C₁₄H₁₇ClN₂O₂
• 分子量: 280.75
• InChiKey: YWEWLRSYNNFWSA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  40.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Pharmacologic inhibition of Myc function
  申请人：——

  公开号：US20040034060A1

  公开（公告）日：2004-02-19

  The c-Myc oncoprotein, a helix-loop-helix-leucine zipper (HLH-ZIP) transcription factor, is frequently deregulated in human cancers. All known functions of c-Myc, including those pertaining to transformation, require that it heterodimerize with another HLH-ZIP protein, Max. Using a high throughput yeast-based assay, we identified seven low molecular weight substances that inhibit c-Myc-Max association. Each compound also prevented this interaction in vitro and inhibited the growth of c-Myc-expressing fibroblasts, although not of fibroblasts lacking c-Myc. Finally, short-term exposure of c-Myc over expressing fibroblasts to several of the compounds markedly reduced their in vivo tumorigenicity. These studies suggest that yeast-based assays can be used to identify inhibitors of protein-protein interactions and that these frequently function in mammalian cells. The signature specificities of each of the c-Myc-Max compounds identified here further suggest synergistic in vivo function.

  c-Myc 癌症蛋白是一种螺旋-环-螺旋-亮氨酸拉链（HLH-ZIP）转录因子，在人类癌症中经常发生失调。c-Myc 的所有已知功能，包括与转化有关的功能，都需要它与另一种 HLH-ZIP 蛋白 Max 异源二聚体。利用基于酵母的高通量试验，我们发现了七种抑制 c-Myc-Max 结合的低分子量物质。每种化合物都能在体外阻止这种相互作用，并抑制表达 c-Myc 的成纤维细胞的生长，但不能抑制缺乏 c-Myc 的成纤维细胞的生长。最后，将过度表达 c-Myc 的成纤维细胞短期暴露于几种化合物中，可明显降低它们在体内的致瘤性。这些研究表明，基于酵母的检测方法可用于鉴定蛋白质-蛋白质相互作用的抑制剂，而且这些抑制剂经常在哺乳动物细胞中发挥作用。这里发现的每种 c-Myc-Max 复合物的特征特异性进一步表明它们在体内具有协同作用。
• LINKED MYC-MAX SMALL MOLECULE INHIBITORS
  申请人：Metallo Steven J.

  公开号：US20120015989A1

  公开（公告）日：2012-01-19

  Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.
• USE OF CYTOPLASMIC C-MYC FOR REGULATING IMMUNE RESPONSES
  申请人：LAU ALLAN SIK YIN

  公开号：US20120107317A1

  公开（公告）日：2012-05-03

  The subject invention provides novel uses of cytoplasmic c-Myc for modulation of innate immune responses. The invention is based, at least in part, on the surprising discovery that cytoplasmic c-Myc, instead of nuclear c-Myc, modulates pro-inflammatory immune responses via its role as a positive feedback regulator. Specifically, the subject invention provides methods for treatment or amelioration of inflammatory diseases and/or immune disorders via inhibition c-Myc expression or its activity. Also provided are methods for the development of therapeutic agents for treating infection, inflammation, immune diseases and autoimmune diseases.
• COMBINATION METHODS FOR TREATMENT OF DISEASE
  申请人：Rahl Peter B.

  公开号：US20130053415A1

  公开（公告）日：2013-02-28

  In some aspects, the invention provides compositions and methods of use for treating a variety of diseases. In some aspect, the compositions and methods involve combined modulation of transcriptional modulators.
• METHODS OF IDENTIFYING AND TREATING IMMUNE CHECKPOINT INHIBITOR-RESPONSIVE NEOPLASMS AND CELLS, TRANSGENIC ANIMALS AND KITS FOR USE THEREIN
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：US20190085404A1

  公开（公告）日：2019-03-21

  Provided are methods of identifying whether a subject having cancer will be responsive to agents that combat immune evasion, such as immune checkpoint inhibitors. Methods of treating a subject having cancer are also provided. Such methods may include those that involve identifying whether the cancer will be responsive to an immune checkpoint inhibitor and/or is an immune-evasive cancer and administering an agent, e.g., an immune checkpoint inhibitor and/or a MYC inhibitor, to the subject to treat the cancer. Also provided are methods of identifying cancer therapeutics that are effective during MYC-regulated immune evasion as well as cancer cell lines and transgenic animals useful in such methods. Kits for use in the described methods are also provided.