4,6-二氯-2-甲基-2H-1-苯并硫嗪-3-甲醛 | 255377-95-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 硫色烯
• 中文名称: 4,6-二氯-2-甲基-2H-1-苯并硫嗪-3-甲醛
• 英文名称: 4,6-dichloro-2-methyl-2H-thiochromene-3-carbaldehyde
• CAS: 255377-95-8
• 化学式: C₁₁H₈Cl₂OS
• mdl: MFCD00220881
• 分子量: 259.2
• InChiKey: DMZWQXPJXXDQLU-UHFFFAOYSA-N

物化性质

• 沸点：
  388.6±42.0 °C(Predicted)
• 密度：
  1.43±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.181
• 拓扑面积：
  42.4
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• PYRROL-1-YL BENZOIC ACID DERIVATIVES USEFUL AS MYC INHIBITORS
  申请人：DANA-FARBER CANCER INSTITUTE, INC.

  公开号：US20150291521A1

  公开（公告）日：2015-10-15

  The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The present invention further provides methods of using the compounds described herein for treating Myc-mediated disorders (e.g., cancer and other proliferative diseases). The present invention also provides assays for identifying Myc inhibitors.

  本发明提供了公式(I-A)、(I-B)和(I-C)的化合物，其药学上可接受的盐以及其制药组合物。本发明的化合物可用于抑制Myc（例如c-Myc）的活性。本发明还提供了使用本文所描述的化合物治疗Myc介导的疾病（例如癌症和其他增殖性疾病）的方法。本发明还提供了用于鉴定Myc抑制剂的检测方法。
• Compositions and methods for treating neoplasia, inflammatory disease and other disorders
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10407441B2

  公开（公告）日：2019-09-10

  The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

  本发明的特点是治疗或预防肿瘤的组合物和方法。 更具体地说，本发明提供了破坏包含溴多聚酶链的 BET 家族多肽与染色质相互作用的组合物和方法（例如，破坏溴多聚酶链与存在于组蛋白 N 端尾上的乙酰-赖氨酸修饰的相互作用）。
• Compositions and methods for treating leukemia
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10676484B2

  公开（公告）日：2020-06-09

  The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.

  本发明提供了用于治疗受试者急性髓性白血病的组合物、方法和试剂盒。
• Bromodomain inhibitor as adjuvant in cancer immunotherapy
  申请人：H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.

  公开号：US10813939B2

  公开（公告）日：2020-10-27

  Inhibition of bromodomain proteins in antigen presenting cells is shown herein to be more inflammatory, to display lower expression of the immunosuppressive molecule PDL1, and to be capable of restoring the responsiveness of tolerant T-cells. Therefore, disclosed is a method for promoting T-cell activation during cancer immunotherapy in a subject that involves administering to a subject undergoing cancer immunotherapy a composition comprising a bromodomain inhibitor. Also disclosed is a method for treating cancer in a subject, comprising co-administering to the subject a bromodomain inhibitor and an immunostimulatory agent.

  本文表明，抑制抗原呈递细胞中的溴化链蛋白会更具有炎症性，显示较低的免疫抑制分子 PDL1 表达，并能够恢复耐受性 T 细胞的反应性。因此，本发明公开了一种在癌症免疫治疗过程中促进受试者 T 细胞活化的方法，该方法包括向接受癌症免疫治疗的受试者施用包含溴链抑制剂的组合物。还公开了一种治疗受试者癌症的方法，该方法包括向受试者联合施用溴链抑制剂和免疫刺激剂。
• Compositions And Methods For Treating Neoplasia, Inflammatory Disease And Other Disorders
  申请人：Bradner James Elliott

  公开号：US20130184264A1

  公开（公告）日：2013-07-18

  The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).