CU-278 | 1013759-88-0

• 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: CU-278
• 英文别名: 2-Amino-4-methoxy-N-(2-methyl-quinolin-8-yl)-benzenesulfonamide；2-amino-4-methoxy-N-(2-methylquinolin-8-yl)benzenesulfonamide
• CAS: 1013759-88-0
• 化学式: C₁₇H₁₇N₃O₃S
• 分子量: 343.406
• InChiKey: OBATTYGMMYIWEY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  103
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  CU-278 在 亚硝酸特丁酯 、 溶剂黄146 作用下， 反应 0.17h， 生成 9-methoxy-3-methyl-5H-quinolino[8,7-c][1,2]benzothiazine 6,6-dioxide
  参考文献：
  名称：

  Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation

  摘要：

  We describe here a series of N-(quinolin-8-yl)benzenesulfonamides capable of suppressing the NF kappa B pathway identified from two high-throughput screens run at two centers of the NIH Molecular Libraries Initiative. These small molecules were confirmed in both primary and secondary assays of NF kappa B activation and expanded upon through analogue synthesis. The series exhibited potencies in the cell-based assays at as low as 0.6 mu M, and several indications suggest that the targeted activity lies within a common region of the NF kappa B pathway. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.10.100
• 作为产物：
  描述：

  2-nitro-4-methoxy-N-(2-methyl-quinolin-8-yl)-benzenesulfonamide 在 tin(ll) chloride 作用下， 以 乙醇 为溶剂， 反应 2.0h， 生成 CU-278
  参考文献：
  名称：

  Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation

  摘要：

  We describe here a series of N-(quinolin-8-yl)benzenesulfonamides capable of suppressing the NF kappa B pathway identified from two high-throughput screens run at two centers of the NIH Molecular Libraries Initiative. These small molecules were confirmed in both primary and secondary assays of NF kappa B activation and expanded upon through analogue synthesis. The series exhibited potencies in the cell-based assays at as low as 0.6 mu M, and several indications suggest that the targeted activity lies within a common region of the NF kappa B pathway. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.10.100

文献信息

• Novel Sulfonaminoquinoline Hepcidin Antagonists
  申请人：Buhr Wilm

  公开号：US20120214803A1

  公开（公告）日：2012-08-23

  The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.

  本发明涉及新型肝铁蛋白拮抗剂，包括它们的药物组合物以及将其用作药物治疗铁代谢紊乱，特别是铁缺乏病和贫血等疾病，特别是与慢性炎症性疾病相关的贫血。
• Sulfonaminoquinoline hepcidin antagonists
  申请人：Vifor (International) AG

  公开号：US09102688B2

  公开（公告）日：2015-08-11

  The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.

  本发明涉及新型的赫普西丁拮抗剂，包括它们的药物组合物和将其作为药物用于治疗铁代谢紊乱的用途，特别是铁缺乏症和贫血，特别是与慢性炎症性疾病相关的贫血。
• NOVEL SULFONAMINOQUINOLINE HEPCIDIN ANTAGONISTS
  申请人：Vifor (International) AG

  公开号：EP2675526B1

  公开（公告）日：2017-02-01
• US9102688B2
  申请人：——

  公开号：US9102688B2

  公开（公告）日：2015-08-11
• Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFκB activity within two separate high-throughput screens of NFκB activation
  作者：Yuli Xie、ShiXian Deng、Craig J. Thomas、Yidong Liu、Ya-Qin Zhang、Alison Rinderspacher、Wenwei Huang、Gangli Gong、Michael Wyler、Efithia Cayanis、Nathalie Aulner、Udo Többen、Caty Chung、Sergey Pampou、Noel Southall、Dušica Vidović、Stephan Schürer、Lars Branden、R. Eric Davis、Louis M. Staudt、James Inglese、Christopher P. Austin、Donald W. Landry、Deborah H. Smith、Douglas S. Auld

  DOI：10.1016/j.bmcl.2007.10.100

  日期：2008.1

  We describe here a series of N-(quinolin-8-yl)benzenesulfonamides capable of suppressing the NF kappa B pathway identified from two high-throughput screens run at two centers of the NIH Molecular Libraries Initiative. These small molecules were confirmed in both primary and secondary assays of NF kappa B activation and expanded upon through analogue synthesis. The series exhibited potencies in the cell-based assays at as low as 0.6 mu M, and several indications suggest that the targeted activity lies within a common region of the NF kappa B pathway. (C) 2007 Elsevier Ltd. All rights reserved.