(4-Benzylpiperazin-1-yl)-acetic acid ethylidene-hydrazide, 5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (4-Benzylpiperazin-1-yl)-acetic acid ethylidene-hydrazide, 5
• 英文别名: 2-(4-benzylpiperazin-1-yl)-N-[(E)-ethylideneamino]acetamide
• 化学式: C₁₅H₂₂N₄O
• 分子量: 274.36
• InChiKey: USXHSONNNDIRCZ-APQPDGGLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  47.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Selective apoptotic induction in cancer cells including activation of procaspase-3
  申请人：The Board of Trustees of the University of Illinois

  公开号：EP2659884A2

  公开（公告）日：2013-11-06

  Compounds and related methods for synthesis, and the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3, and particular embodiments are capable of direct activation of procaspase-3 and procaspase-7 to the effector forms of caspase-3 and caspase-7. Procaspase-3 levels can vary among cancer cell types; several types have relatively high levels and can have increased susceptibility to chemotherapy by compounds and methods herein. Therapeutic applications are relevant for a variety of cancer conditions and cell types, e.g. breast, lung, brain, colon, renal, adrenal, melanoma, and others.

  公开了化合物和相关的合成方法，以及化合物在治疗癌症和选择性诱导细胞凋亡疗法中的用途。所公开的化合物涉及对原蛋白酶（如原蛋白酶-3）的修饰，特定的实施方案能够将原蛋白酶-3和原蛋白酶-7直接激活为caspase-3和caspase-7的效应形式。Procaspase-3 的水平可因癌细胞类型而异；有几种癌细胞类型的 Procaspase-3 水平相对较高，可增加对本文所述化合物和方法化疗的敏感性。治疗应用适用于多种癌症病症和细胞类型，如乳腺癌、肺癌、脑癌、结肠癌、肾癌、肾上腺癌、黑色素瘤等。
• Compounds and methods for the treatment of cancer
  申请人：The Board of Trustees of the University of Illinois

  公开号：US10166229B2

  公开（公告）日：2019-01-01

  Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.

  在有关诱导细胞死亡（如癌细胞）的实施方案中，公开了化合物和方法。公开了化合物及其合成和使用的相关方法，包括在治疗癌症和选择性诱导细胞凋亡的疗法中使用化合物。所公开的化合物涉及对原蛋白酶（如原蛋白酶-3）的修饰。在实施方案中，组合物能够激活procaspase-3。
• SELECTIVE APOPTOTIC INDUCTION IN CANCER CELLS INCLUDING ACTIVATION OF PROCASPASE-3
  申请人：THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

  公开号：EP1893210B1

  公开（公告）日：2019-10-02
• Selective Apoptotic Induction in Cancer Cells Including Activation of Procaspase-3
  申请人：Hergenrother J. Paul

  公开号：US20070049602A1

  公开（公告）日：2007-03-01

  Compounds and related methods for synthesis, and the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3, and particular embodiments are capable of direct activation of procaspase-3 and procaspase-7 to the effector forms of caspase-3 and caspase-7. Procaspase-3 levels can vary among cancer cell types; several types have relatively high levels and can have increased susceptibility to chemotherapy by compounds and methods herein. Therapeutic applications are relevant for a variety of cancer conditions and cell types, e.g. breast, lung, brain, colon, renal, adrenal, melanoma, and others.
• Compositions and Methods Including Cell Death Inducers and Procaspase Activation
  申请人：HERGENROTHER Paul J.

  公开号：US20110257398A1

  公开（公告）日：2011-10-20

  Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.