N-benzyl-2-[(3Z)-6-fluoro-2-methyl-3-[(3,4,5-trimethoxyphenyl)methylidene]inden-1-yl]acetamide | 200803-37-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚和异茚
• 英文名称: N-benzyl-2-[(3Z)-6-fluoro-2-methyl-3-[(3,4,5-trimethoxyphenyl)methylidene]inden-1-yl]acetamide
• CAS: 200803-37-8
• 化学式: C₂₉H₂₈FNO₄
• 分子量: 473.5
• InChiKey: KATLSKIJHJJAEB-FMCGGJTJSA-N

物化性质

• 沸点：
  667.3±55.0 °C(Predicted)
• 密度：
  1.206±0.06 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  56.8
• 氢给体数：
  1
• 氢受体数：
  5

制备方法与用途

生物活性

OSIP-486823 是一种新型的微管干扰剂，对蛋白激酶 G (PKG) 和微管均具有生物学作用。

靶点

Microtubule

体外研究

OSIP486823 inhibits growth and induce apoptosis in SW480 human colon cancer cells, with IC ₅₀ of 0.1 μM. OSIP-486823 (OSIP486823) causes depolymerization of microtubules in interphase cells, inhibit spindle formation in mitotic cells, and induce multinucleated cells. Exisulind and the potent synthetic derivative OSIP-486823 are members of a new class of drugs known as selective apoptotic antineoplastic drugs that target cyclic guanosine 3′,5′-monophosphate phosphodiesterases (cGMP-PDE). OSIP-486823 also disrupts microtubule polymerization, perturbs mitotic spindle function, and arrests cells in mitosis in human glioma cells.

文献信息

• INDENYL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND MEDICAL USES THEREOF
  申请人：ADT PHARMACEUTICALS, INC.

  公开号：US20160168113A1

  公开（公告）日：2016-06-16

  Disclosed are compounds, for example, compounds of formula I, wherein R, R 0 , R 1 -R 8 , n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

  揭示了化合物，例如，具有公式I的化合物，其中R、R0、R1-R8、n、X、Y、Y′和E如本文所述，包含这些化合物的药物组合物，以及治疗或预防疾病或病症的方法，例如癌症。
• METHOD OF TREATING OR PREVENTING RAS-MEDIATED DISEASES
  申请人：ADT PHARMACEUTICALS, INC.

  公开号：US20160168108A1

  公开（公告）日：2016-06-16

  Disclosed are compounds, for example, a compound of formula I, wherein R, R 0 , R 1 -R 8 , n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.

  揭示了化合物，例如，公式I的化合物，其中R、R0、R1-R8、n、X、Y、Y′和E如本文所述，包含这些化合物的药物组合物，以及治疗或预防疾病或状况的方法，例如由ras基因介导的癌症。
• Anticancer indenes, indanes, azaindenes, azaindanes, pharmaceutical compositions and uses
  申请人：ADT PHARMACEUTICALS, LLC

  公开号：US11186596B2

  公开（公告）日：2021-11-30

  Disclosed are compounds for medical uses, for example, compounds of formula (Ia), wherein A1, A2, A3, A4, A5, A6, A7, R6, R7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

  公开了用于医疗用途的化合物，例如式（Ia）化合物（其中 A1、A2、A3、A4、A5、A6、A7、R6、R7 和 E 如本文所述）、含有此类化合物的药物组合物，以及治疗或预防疾病或病症（例如癌症）的方法。
• Method of treating or preventing Ras-mediated diseases
  申请人：ADT Pharmaceuticals, LLC

  公开号：US11198679B2

  公开（公告）日：2021-12-14

  Disclosed are compounds, for example, a compound of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.

  本发明公开了化合物，例如，具有式I的化合物，其中R、R0、R1-R8、n、X、Y、Y’和E如本文所述，含有此类化合物的药物组合物，以及用于治疗或预防由ras基因介导的疾病或病症（例如癌症）的方法。
• Composition comprising a pde4 inhibitor and a pde5 inhibitor
  申请人：Dunkern Torsten

  公开号：US20060094723A1

  公开（公告）日：2006-05-04

  The invention relates to the combined administration of a PDE4 inhibitor and a PDE5 inhibitor for the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.

  本发明涉及联合使用 PDE4 抑制剂和 PDE5 抑制剂治疗磷酸二酯酶 4（PDE4）和/或磷酸二酯酶 5（PDE5）有害的疾病。