(E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1,2-diphenylethyl)acrylamide | 1001088-89-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1,2-diphenylethyl)acrylamide
• 英文别名: (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1,2-diphenylethyl)prop-2-enamide
• CAS: 1001088-89-6
• 化学式: C₂₃H₁₈BrN₃O
• 分子量: 432.319
• InChiKey: IPRQXTJFBOZPBC-XDJHFCHBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  65.8
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• TRYPHOSTIN-ANALOGS FOR THE TREATMENT OF CELL PROLIFERATIVE DISEASES
  申请人：Donato Nicholas J

  公开号：US20100292229A1

  公开（公告）日：2010-11-18

  The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.

  本发明涉及化合物及其用于治疗细胞增殖性疾病，如癌症。在一般方面，本发明的化合物在结构上类似于酪氨酸激酶抑制剂。在某些实施例中，本发明的化合物通过诱导应激颗粒结合特定信号分子并阻止它们参与信号转导和肿瘤发生，从而表现出显著的效力，例如抑制Stat3激活、降低c-myc蛋白水平和/或诱导肿瘤细胞凋亡。在一般方面，本发明的化合物在纳摩尔浓度下诱导这些活性中的一个或多个，并通常通过诱导应激颗粒的独特机制发挥作用，这些应激颗粒结合特定信号分子并防止它们参与信号转导和肿瘤发生。
• METHODS OF TREATING DERMATOLOGIC, GYNECOLOGIC, AND GENITAL DISORDERS WITH CAFFEIC ACID ANALOGS
  申请人：Priebe Anna

  公开号：US20110275577A1

  公开（公告）日：2011-11-10

  The present invention relates to caffeic acid analog compounds and methods which may be useful for regeneration, cellular programming, and the treatment of dermatologic, gynecologic, and genital diseases such as inflammatory dermatologic conditions, dysplasia, neoplasia, in situ carcinoma, invasive carcinoma, lichen sclerosus, lichen planus, vaginal dysplasia, vaginal carcinoma, vulvar dysplasia, vulvar carcinoma, cervical dysplasia, cervical carcinoma, and Kaposi's sarcoma.
• INTERFERON THERAPIES IN COMBINATION WITH BLOCKADE OF STAT3 ACTIVATION
  申请人：Priebe Waldemar

  公开号：US20130129675A1

  公开（公告）日：2013-05-23

  Methods of modulating the INF-induced STAT3 activation in a patient in need-thereof are provided for the treatment of disease. The methods comprise the step of administrating to a patient the combination of a therapeutically effective amount of interferon including INF-α and/or INF-β in combination with a STAT3 inhibitor.
• [EN] SIGNALING PROTEIN MODULATORS AS THERAPEUTIC AGENTS<br/>[FR] MODULATEURS DE PROTÉINE SIGNAL EN TANT QU'AGENTS THÉRAPEUTIQUES
  申请人：UNIV TEXAS

  公开号：WO2008005954A2

  公开（公告）日：2008-01-10

  [EN] The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.
  [FR] La présente invention concerne des composés et leur utilisation pour traiter des maladies associées à la prolifération cellulaire telles que le cancer. En général, les composés de la présente invention présentent une structure de type tyrphostine. Selon certains modes de réalisation, les composés de la présente invention font preuve d'un pouvoir significatif en provoquant, par exemple, l'inhibition de l'activation des protéines Stat3, la réduction des niveaux de protéines c-myc et/ou l'induction de l'apoptose de cellules tumorales. En général, les composés de la présente invention induisent une ou plusieurs de ces activités à des concentrations nanomolaires et ils agissent généralement selon un mécanisme unique impliquant l'induction de granules de stress qui se lient à des molécules de signal spécifiques et les empêchent de participer à la transduction du signal et à l'oncogenèse.