5-(5-Pyridin-3-yl-pent-4-ynyl)-5-(toluene-4-sulfonyl)thiazolidine-2,4-dione | 500710-59-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-(5-Pyridin-3-yl-pent-4-ynyl)-5-(toluene-4-sulfonyl)thiazolidine-2,4-dione
• 英文别名: 5-(5-Pyridin-3-yl-pent-4-ynyl)-5-(toluene-4-sulfonyl)-thiazolidine-2,4-dione；5-(4-methylphenyl)sulfonyl-5-(5-pyridin-3-ylpent-4-ynyl)-1,3-thiazolidine-2,4-dione
• CAS: 500710-59-8
• 化学式: C₂₀H₁₈N₂O₄S₂
• 分子量: 414.506
• InChiKey: MPFPNIKGPDPQDN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  127
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  5-pent-4-ynyl-5-(toluene-4-sulfonyl)-thiazolidine-2,4-dione 、 4-戊炔-1-醇 、 、 二乙胺 在 碘化亚铜 氮气 作用下， 以 二氯甲烷 为溶剂， 反应 72.0h， 以to give the title compound as a light beige solid, mp 173-176° C., THEORY的产率得到5-(5-Pyridin-3-yl-pent-4-ynyl)-5-(toluene-4-sulfonyl)thiazolidine-2,4-dione
  参考文献：
  名称：

  Method of using 5-(arysulfonyl)-, 5-(arylsulfanyl)-and 5-(arylsulfanyl)thiazolidine-2,4-diones for inhibition of farnesyl-protein transferase

  摘要：

  本发明涉及一种使用新型5-(芳基磺酰基)-5-(芳基亚磺酰基)-和5-(芳基硫基)噻唑烷-2,4-二酮（式I），其中Ar、Ar'、R6、m和n如规范中所定义的抑制Ras FPTase的方法，可用作替代或与传统癌症治疗结合治疗ras-癌基因依赖性肿瘤，如胰腺癌、结肠癌、膀胱癌和甲状腺癌。

  公开号：

  US06605628B1

文献信息

• Method of using 5-(arysulfonyl)-, 5-(arylsulfanyl)-and 5-(arylsulfanyl)thiazolidine-2,4-diones for inhibition of farnesyl-protein transferase
  申请人：American Cyanamid Company

  公开号：US20030144301A1

  公开（公告）日：2003-07-31

  This invention relates to a method of using novel 5-(arylsulfonyl)-, 5-(arylsulfinyl)- and 5-(arylsulfanyl)thiazolidine-2,4-diones of Formula (1), wherein Ar, Ar′, R 6 , m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras- oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid. 1

  这项发明涉及使用新型5-(芳基磺酰基)-、5-(芳基亚砜基)-和5-(芳基硫基)噻唑烷-2,4-二酮的方法，其化学式如下(1)，其中Ar、Ar′、R6、m和n如规范中定义的作为Ras FPTase的抑制剂，并可作为传统癌症治疗的替代方案或与之结合，用于治疗Ras-致癌基因依赖性肿瘤，如胰腺癌、结肠癌、膀胱癌和甲状腺癌。
• 5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones useful for inhibition of farnesyl-protein transferase
  申请人：American Cyanamid Company

  公开号：US20030149063A1

  公开（公告）日：2003-08-07

  This invention relates to a method of using novel 5-(arylsulfonyl)-,5- (arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R 6 , m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras- oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid. 1

  本发明涉及一种使用新型5-(芳基磺酰基)-、5-(芳基亚磺酰基)和5-(芳基硫基)-噻唑烷-2,4-二酮（式（I）中的Ar、Ar'、R6、m和n如规范中定义）作为Ras FPTase抑制剂的方法，可用作替代传统癌症治疗或与之结合治疗ras-oncogene依赖性肿瘤，例如胰腺癌、结肠癌、膀胱癌和甲状腺癌。
• US6605628B1
  申请人：——

  公开号：US6605628B1

  公开（公告）日：2003-08-12
• US6784184B2
  申请人：——

  公开号：US6784184B2

  公开（公告）日：2004-08-31
• [EN] METHOD OF USING 5-(ARYLSULFONYL)-,5-(ARYLSULFINYL), AND 5-(ARYLSULFANYL)-THIAZOLIDINE-2,4-DIONES FOR INHIBITION OF FARNESYL-PROTEIN TRANSFERASE<br/>[FR] PROCEDE D'UTILISATION DE 5-(ARYLSULFONYLE)-,5-(ARYLSULFINYLE), ET 5-(ARYLSULFANYLE)-THIAZOLIDINE-2,4-DIONES POUR L'INHIBITION DE LA FARNESYLE-PROTEINE TRANSFERASE
  申请人：WYETH CORP

  公开号：WO2003018135A1

  公开（公告）日：2003-03-06

  This invention relates to novel 5-(arylsulfonyl)-thiazolidine-2,4-diones, and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar', R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras-oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid, to processes for the preparation of such compounds, and pharmaceutical compositions containing them.