(Z)-5-(4-phenoxyphenyl)methylidene-2-thioxo-4-thiazolidinone | 1266332-07-3

• 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: (Z)-5-(4-phenoxyphenyl)methylidene-2-thioxo-4-thiazolidinone
• 英文别名: (5Z)-5-[(4-phenoxyphenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one
• CAS: 1266332-07-3
• 化学式: C₁₆H₁₁NO₂S₂
• 分子量: 313.401
• InChiKey: DNXCXYIPCYQEBG-UVTDQMKNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  95.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (Z)-5-(4-phenoxyphenyl)methylidene-2-thioxo-4-thiazolidinone 、 sodium hydroxide 、 盐酸 生成 3-(4-phenoxyphenyl)-2-thioxopropionic acid
  参考文献：
  名称：

  TOMISAWA, KAZUYUKI;KAMEO, KAZUYA;MATSUNAGA, TOHRU;SAITO, SHIUJI;HOSODA, K+, CHEM. AND PHARM. BULL., 1986, 34, N 2, 701-712

  摘要：

  DOI：
• 作为产物：
  描述：

  罗丹宁 、 4-苯氧基苯甲醛 在 sodium acetate 作用下， 以 溶剂黄146 为溶剂， 以70%的产率得到(Z)-5-(4-phenoxyphenyl)methylidene-2-thioxo-4-thiazolidinone
  参考文献：
  名称：

  In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors

  摘要：

  2-Thioxo-4-thiazolidinone derivatives were evaluated as aldose reductase inhibitors (ARIs) and most of them exhibited good or excellent in vitro efficacy. Out of the tested compounds, most N-unsubstituted analogues were found to possess inhibitory effects at low micromolar doses and two of them exhibited higher potency than sorbinil, used as a reference drug. The insertion of an acetic chain on N-3 of the thiazolidinone scaffold led to analogues with submicromolar affinity for ALR2 and IC50 values very similar to that of epalrestat, the only ARI currently used in therapy. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.11.041

文献信息

• [EN] INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX AND METHODS FOR USE OF THE SAME<br/>[FR] INHIBITEURS DU COMPLEXE D'ACTIVATION DE TRANSCRIPTION DU RÉCEPTEUR NOTCH ET PROCÉDÉS D'UTILISATION DE CES DERNIERS
  申请人：UNIV MIAMI

  公开号：WO2016154255A1

  公开（公告）日：2016-09-29

  Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

  本文披露了Notch转录激活复合物的抑制剂，以及它们在治疗或预防疾病（如癌症）中的使用方法。本文描述的抑制剂可以包括式（I）的化合物及其药用可接受盐：式（I），其中取代基如所述。
• Inhibitors of the Notch transcriptional activation complex and methods for use of the same
  申请人：UNIVERSITY OF MIAMI

  公开号：US10501413B2

  公开（公告）日：2019-12-10

  Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

  本文公开了 Notch 转录激活复合物的抑制剂，以及将其用于治疗或预防癌症等疾病的方法。本文所述的抑制剂可包括式（I）化合物及其药学上可接受的盐类：式 (I)，其中取代基如所述。
• INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX AND METHODS FOR USE OF THE SAME
  申请人：SPYVEE Mark

  公开号：US20180086700A1

  公开（公告）日：2018-03-29

  Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.
• In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors
  作者：Rosanna Maccari、Antonella Del Corso、Marco Giglio、Roberta Moschini、Umberto Mura、Rosaria Ottanà

  DOI：10.1016/j.bmcl.2010.11.041

  日期：2011.1

  2-Thioxo-4-thiazolidinone derivatives were evaluated as aldose reductase inhibitors (ARIs) and most of them exhibited good or excellent in vitro efficacy. Out of the tested compounds, most N-unsubstituted analogues were found to possess inhibitory effects at low micromolar doses and two of them exhibited higher potency than sorbinil, used as a reference drug. The insertion of an acetic chain on N-3 of the thiazolidinone scaffold led to analogues with submicromolar affinity for ALR2 and IC50 values very similar to that of epalrestat, the only ARI currently used in therapy. (C) 2010 Elsevier Ltd. All rights reserved.
• TOMISAWA, KAZUYUKI;KAMEO, KAZUYA;MATSUNAGA, TOHRU;SAITO, SHIUJI;HOSODA, K+, CHEM. AND PHARM. BULL., 1986, 34, N 2, 701-712
  作者：TOMISAWA, KAZUYUKI、KAMEO, KAZUYA、MATSUNAGA, TOHRU、SAITO, SHIUJI、HOSODA, K+

  DOI：——

  日期：——