GTP-4 | 808196-22-7

• 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: GTP-4
• 英文别名: [(2S,3R)-3-(3,4,5-trihydroxybenzoyl)oxy-1,2,3,4-tetrahydronaphthalen-2-yl] 3,4,5-trihydroxybenzoate
• CAS: 808196-22-7
• 化学式: C₂₄H₂₀O₁₀
• 分子量: 468.417
• InChiKey: TZXFQPGYJRKWOC-BGYRXZFFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  34
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  174
• 氢给体数：
  6
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  GTP-4 、 乙酸酐 在 吡啶 作用下， 以94%的产率得到[(2S,3R)-3-(3,4,5-triacetyloxybenzoyl)oxy-1,2,3,4-tetrahydronaphthalen-2-yl] 3,4,5-triacetyloxybenzoate
  参考文献：
  名称：

  Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs

  摘要：

  A pro-drug 8 of a synthetic analog 7 is more active in its antiproliferative activity against human breast cancer MDA-MB-231 cells possessing high catechol-O-methyltransferase (COMT) activity than the prodrugs of EGCG and the analog 5. The higher activity of 8 is attributed to it not being a substrate of COMT. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2009.12.034
• 作为产物：
  描述：

  (2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-tris(benzyloxy)benzoate) 在 20% palladium hydroxide on carbon 、 氢气 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 以95%的产率得到GTP-4
  参考文献：
  名称：

  Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs

  摘要：

  A pro-drug 8 of a synthetic analog 7 is more active in its antiproliferative activity against human breast cancer MDA-MB-231 cells possessing high catechol-O-methyltransferase (COMT) activity than the prodrugs of EGCG and the analog 5. The higher activity of 8 is attributed to it not being a substrate of COMT. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2009.12.034

文献信息

• Polyphenol proteasome inhibitors, synthesis, and methods of use
  申请人：Dou Q. Ping

  公开号：US20100173985A1

  公开（公告）日：2010-07-08

  The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

  本发明涉及合成的绿茶多酚化合物、它们的合成方式以及它们在抑制蛋白酶体活性和治疗癌症方面的应用。本发明还涉及制药组合物，用于抑制蛋白酶体和治疗癌症的方法。
• POLYPHENOL PROTEASOME INHIBITORS, SYNTHESIS, AND METHODS OF USE
  申请人：UNIVERSITY OF SOUTH FLORIDA

  公开号：US20140045931A1

  公开（公告）日：2014-02-13

  The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

  本发明涉及合成绿茶多酚化合物及其合成方式，以及它们在抑制蛋白酶体活性和治疗癌症方面的应用。本发明还涉及制备药物组合物，用于抑制蛋白酶体和治疗癌症的方法。
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