N-methyl-4-(4-(phenylsulfonamido)phenoxy)picolinamide | 1313019-66-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-methyl-4-(4-(phenylsulfonamido)phenoxy)picolinamide
• 英文别名: 4-[4-(benzenesulfonamido)phenoxy]-N-methylpyridine-2-carboxamide
• CAS: 1313019-66-7
• 化学式: C₁₉H₁₇N₃O₄S
• 分子量: 383.428
• InChiKey: AUUBJPHZBKJLMV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  106
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4-氯-2-吡啶羰酰氯盐酸盐 在 吡啶 、 potassium tert-butylate 作用下， 以 四氢呋喃 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 22.44h， 生成 N-methyl-4-(4-(phenylsulfonamido)phenoxy)picolinamide
  参考文献：
  名称：

  [EN] KINASE INHIBITOR COMPOUNDS, COMPOSITIONS, AND METHODS OF TREATING CANCER
  [FR] COMPOSÉS INHIBITEURS DE KINASE, COMPOSITIONS ET MÉTHODES DE TRAITEMENT DU CANCER

  摘要：

  公开号：

  WO2018035346A8

文献信息

• [EN] AGONISTS OF SRC HOMOLOGY-2 CONTAINING PROTEIN TYROSINE PHOSPHATASE-1 AND TREATMENT METHODS USING THE SAME<br/>[FR] AGONISTES DE PROTÉINE TYROSINE PHOSPHATASE-1 CONTENANT UN DOMAINE D'HOMOLOGIE SRC-2 ET PROCÉDÉS DE TRAITEMENT L'EMPLOYANT
  申请人：UNIV NAT TAIWAN

  公开号：WO2013020014A1

  公开（公告）日：2013-02-07

  The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase- 1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.

  本发明提供了式I、II或III的新化合物，这些化合物具有Src同源-2含有蛋白酪氨酸磷酸酶-1（SHP-1）激动剂活性。同时，本发明还提供了使用式I、II或III的化合物进行治疗的方法。
• Kinase inhibitor compounds, compositions, and methods of treating cancer
  申请人：ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

  公开号：US10519113B2

  公开（公告）日：2019-12-31

  The present invention relates to a compound having the structure of formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where X, Y, Z, R, R1, R2, R3, R4, R5, and R6 are as described herein. The present invention also relates to compositions containing the compound having the structure of formula (I), and a method of treating cancer in a subject.

  本发明涉及一种具有式（I）结构的化合物或其立体异构体、药学上可接受的盐、氧化物或溶液，其中 X、Y、Z、R、R1、R2、R3、R4、R5 和 R6 如本文所述。本发明还涉及含有具有式（I）结构的化合物的组合物，以及治疗受试者癌症的方法。
• Sorafenib derivatives induce apoptosis through inhibition of STAT3 independent of Raf
  作者：Kuen-Feng Chen、Wei-Tien Tai、Jui-Wen Huang、Cheng-Yi Hsu、Wei-Lin Chen、Ann-Lii Cheng、Pei-Jer Chen、Chung-Wai Shiau

  DOI：10.1016/j.ejmech.2011.04.007

  日期：2011.7

  STAT3 is a transcription factor that modulates survival-directed transcription. It is persistently activated in many human cancers. Literature has shown that sorafenib, Raf kinase inhibitor, reduces Phospho-STAT3 and induces cell death. A series of sorafenib derivatives were synthesized as new inhibitors for STAT3. Urea, sulfonamide, and carboxamide linkers brought out different SARs from the end of sorafenib. Urea and carboxamide linked derivatives showed greater inhibition against STAT3 activity than sulfonamide linked derivatives. In particular, 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy) phenyl)urea (1), a urea linker, was as potent as sorafenib in reducing P-STAT3 level and cell death but no inhibition for Raf activity. Such result provides a new lead for the design of STAT3 inhibitors. (C) 2011 Elsevier Masson SAS. All rights reserved.
• AGONISTS OF SRC HOMOLOGY-2 CONTAINING PROTEIN TYROSINE PHOSPHATASE-1 AND TREATMENT METHODS USING THE SAME
  申请人：National Taiwan University

  公开号：EP2739139B1

  公开（公告）日：2019-09-25
• KINASE INHIBITOR COMPOUNDS, COMPOSITIONS, AND METHODS OF TREATING CANCER
  申请人：ICHAN SCHOOL OF MEDICINE AT MOUNT SINAI

  公开号：US20190202789A1

  公开（公告）日：2019-07-04

  The present invention relates to a compound having the structure of formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where X, Y, Z, R, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as described herein. The present invention also relates to compositions containing the compound having the structure of formula (I), and a method of treating cancer in a subject.