cis-PtCl2(NH2CH3)(aminoethanol) | 868602-78-2

• 英文名称: cis-PtCl2(NH2CH3)(aminoethanol)
• CAS: 868602-78-2
• 化学式: C₃H₁₂Cl₂N₂OPt
• 分子量: 358.127
• InChiKey: OBBUQMDVFYXSDR-UHFFFAOYSA-L

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：

  guanosine 5'-monophosphate 、 cis-PtCl2(NH2CH3)(aminoethanol) 以 N,N-二甲基甲酰胺-d7 为溶剂， 生成
  参考文献：
  名称：

  Structure–activity relationship studies for three new asymmetric cis-platinum(II) aminoethanol-based complexes

  摘要：

  The design and synthesis of three asymmetrical platinum(II) analogues of cisplatin with substituents on the amine, varying in polarity and steric bulk is presented. Their biological activities, as studied using in vitro cytotoxicity studies in cisplatin sensitive and the corresponding cisplatin resistant cell lines, cellular uptake experiments and in a reaction with model DNA base GMP, are presented. All compounds exhibit promising cytotoxicity in the cisplatin sensitive cell lines albeit lower than cisplatin. On the other hand, the complexes partly overcome cisplatin resistance in the resistant cell lines. A direct correlation between cytotoxicity and cellular uptake was found. Conversely, the rate of reaction of all compounds with the model base GMP was found to be very similar and faster than cisplatin. It was therefore concluded that the difference in activity observed for these complexes is due to differential cellular uptake rather than the reactivity towards the cellular target of platinum complexes, nuclear DNA. (c) 2006 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.ica.2006.05.011
• 作为产物：
  描述：

  trans-[bis(μ-iodo)diiodobis(methylamino)diplatinum(II)] 、 potassium chloride 、 C.I.酸性橙108 在 silver nitrate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以89%的产率得到cis-PtCl2(NH2CH3)(aminoethanol)
  参考文献：
  名称：

  Structure–activity relationship studies for three new asymmetric cis-platinum(II) aminoethanol-based complexes

  摘要：

  The design and synthesis of three asymmetrical platinum(II) analogues of cisplatin with substituents on the amine, varying in polarity and steric bulk is presented. Their biological activities, as studied using in vitro cytotoxicity studies in cisplatin sensitive and the corresponding cisplatin resistant cell lines, cellular uptake experiments and in a reaction with model DNA base GMP, are presented. All compounds exhibit promising cytotoxicity in the cisplatin sensitive cell lines albeit lower than cisplatin. On the other hand, the complexes partly overcome cisplatin resistance in the resistant cell lines. A direct correlation between cytotoxicity and cellular uptake was found. Conversely, the rate of reaction of all compounds with the model base GMP was found to be very similar and faster than cisplatin. It was therefore concluded that the difference in activity observed for these complexes is due to differential cellular uptake rather than the reactivity towards the cellular target of platinum complexes, nuclear DNA. (c) 2006 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.ica.2006.05.011