| 1380079-66-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• CAS: 1380079-66-2
• 化学式: C₂₈H₄₁I₂N₃O₄Si₂
• 分子量: 793.631
• InChiKey: SGYIIUWBGIZNCD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
  None
• 可旋转键数：
  None
• 环数：
  None
• sp3杂化的碳原子比例：
  None
• 拓扑面积：
  None
• 氢给体数：
  None
• 氢受体数：
  None

反应信息

• 作为反应物：
  描述：

  在 四丁基氟化铵 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 以60%的产率得到3-(1-(3,5-diiodo-4-methoxyphenyl)-1H-1,2,3-triazol-5-yl)-6-methoxybenzene-1,2-diol
  参考文献：
  名称：

  Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A–1

  摘要：

  The antiproliferative activity on ovarian cancer (SK-OV-3) cells of a series of triazole-bridged combretastatin analogues (37, 38, 40-43) containing dihalogenation of the A-ring is reported, and compared with their trimethoxy analogues (5, 15, 39). It was found that dihalogenation with either bromine or iodine was a tolerated modification when compared to the parent compound combretastatin (CA-4, 1) and had less effect than B-ring modification on potency. These compounds exhibited G(2)/M arrest, and maintained antitubulin activity. Further assays on human umbilical vein endothelial cells (HUVECs) demonstrated the potential antivascular effects of these triazoles. Of particular note was a 3,5-diiodo-4-methoxyaryl triazole (43) which had promising 7-fold selectivity for HUVECs over ovarian cancer cells. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.01.010
• 作为产物：
  描述：

  2,6-二碘-4-硝基苯酚 在 盐酸 、 乙醇 、 乙基氯化镁 、 potassium carbonate 、 tin(ll) chloride 、 sodium nitrite 作用下， 以 四氢呋喃 、 水 、 乙酸乙酯 、 丙酮 为溶剂， 反应 26.5h， 生成
  参考文献：
  名称：

  Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A–1

  摘要：

  The antiproliferative activity on ovarian cancer (SK-OV-3) cells of a series of triazole-bridged combretastatin analogues (37, 38, 40-43) containing dihalogenation of the A-ring is reported, and compared with their trimethoxy analogues (5, 15, 39). It was found that dihalogenation with either bromine or iodine was a tolerated modification when compared to the parent compound combretastatin (CA-4, 1) and had less effect than B-ring modification on potency. These compounds exhibited G(2)/M arrest, and maintained antitubulin activity. Further assays on human umbilical vein endothelial cells (HUVECs) demonstrated the potential antivascular effects of these triazoles. Of particular note was a 3,5-diiodo-4-methoxyaryl triazole (43) which had promising 7-fold selectivity for HUVECs over ovarian cancer cells. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.01.010

文献信息

• Kojic acid-amino acid amide metal complexes and their melanogenesis inhibitory activities
  作者：Seon-Yeong Kwak、Hye-Ryung Choi、Kyoung-Chan Park、Yoon-Sik Lee

  DOI：10.1002/psc.1404

  日期：2011.12

  and prevent enzymatic browning in food. Previously, we reported that kojic acid–amino acid amide (KA‐AA‐NH2) showed enhanced tyrosinase inhibitory activity compared with kojic acid alone, but this was not observed in a cell test because of poor cell permeability. To enhance cell permeability, we prepared copper and zinc complexes of KA‐AA‐NH2 and characterized them using FT‐IR spectroscopy, ESI‐MS

  酪氨酸酶通过催化底物的氧化在黑色素合成途径的早期发挥关键作用。因此，已经在化妆品和食品工业中对酪氨酸酶抑制剂进行了深入研究，以开发色素不足剂并防止食品中的酶促褐变。以前，我们报道了曲酸-氨基酸酰胺（KA-AA-NH 2）与单独的曲酸相比显示出增强的酪氨酸酶抑制活性，但由于细胞通透性差，在细胞试验中未观察到。为了提高细胞通透性，我们制备了KA‐AA‐NH 2的铜和锌配合物，并使用FT‐IR光谱，ESI‐MS光谱和电感耦合等离子体分析对其进行了表征。然后我们证明KA‐AA‐NH 2铜配合物在Mel-Ab细胞中表现出黑色素生成抑制活性。版权所有©2011欧洲肽协会和John Wiley＆Sons，Ltd.。