trans-dihydroxo-diammine-platinum(II) | 63700-88-9

• 英文名称: trans-dihydroxo-diammine-platinum(II)
• 英文别名: trans-Dihydroxo-diammin-platin(II)；azane;platinum(2+);dihydroxide
• CAS: 63700-88-9
• 化学式: H₈N₂O₂Pt
• 分子量: 263.156
• InChiKey: XXESGWORFDGSQY-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：

  trans-dihydroxo-diammine-platinum(II) 在 盐酸 作用下， 以 盐酸 为溶剂， 生成 transplatin
  参考文献：
  名称：

  Ryabchikov, D. I., 1935, # IV, p. 259 - 262

  摘要：

  DOI：
• 作为产物：
  描述：

  transplatin 在 sodium hydroxide 作用下， 以 水 为溶剂， 生成 trans-dihydroxo-diammine-platinum(II)
  参考文献：
  名称：

  The hydrolysis products of cis-diamminedichloroplatinum(II) 6. A kinetic comparison of the cis- and trans-isomers and other cis-di(amine)di(chloro)platinum(II) compounds

  摘要：

  Di(amine)di(chloro)platinum(II) complexes react in aqueous acid solution to form an equilibrium mixture L2PtCl2 k-1 reversible kj L2PtCl(OH2)+ + Cl-. Values of k1, K-1 and the equilibrium constant K(T) (-k1/k-1) have been measured for the systems L2 = cis(NH3)2, trans(NH3)2, cis(py)2, en, RR-chxn, tn and Me2tn, with varying temperature and ionic strength (cis(NH3)2 only). At 25-degrees-C and I = 0.1 M, data for cis-PtCl2(NH3)2 are k1 = 5.18 x 10(-5) s-1 (DELTA-H# = 86.7 kJ mol-1, DELTA-S# = -36 J K mol-1), k1 = 7.68 x 10(-3) M-1 s-1 (DELTA-H# - 72.7, DELTA-S# = - 41) and K1 = 6.74 x 10(-3). Corresponding data for trans-PtCl2(NH3)2 are k1 = 1.90 x 10(-5) s-1 (DELTA-H# = 92.2, DELTA-S# = - 26), k-1 - 3.05 x 10(-2) M-1 s-1 (DELTA-H# = 85.7, DELTA-S# = + 14) and K1 = 6.22 x 10(-4). These data provide a kinetic explanation for the inactivity of the trans-isomer as an anti-cancer drug.

  DOI：

  10.1016/s0020-1693(00)80242-x

文献信息

• SYNTHESIS OF (GLYCOLATO-<i>O</i>,<i>O</i>′)DIAMMINEPLATINUM(II) AND ITS RELATED COMPLEXES
  作者：Tetsushi Totani、Katsutoshi Aono、Michihiro Komura、Yasuko Adachi

  DOI：10.1246/cl.1986.429

  日期：1986.3.5

  Glycolatoplatinum(II) complexes, [Pt(OCOCH2O)L2], having a novel five-membered ring structure were obtained by adding an equimolar quantity of glycolic acid to cis-[Pt(OH)2L2] (L: NH3, amines) in water followed by heating. These complexes have also been obtained by reaction of cis-[Pt(NO3)2L2] with sodium glycolate in neutral aqueous solution. These complexes have been characterized by SIMS, IR, and NMR spectroscopy.

  甘醇酸合铂(II)配合物[Pt(OCOCH2O)L2]是一种具有新型五元环结构的化合物，通过将甘醇酸与水合顺式-[Pt(OH)2L2]（L：NH3、胺）等摩尔比混合并在水中加热制得。这些配合物也可通过顺式-[Pt(NO3)2L2]与甘醇酸钠在中性水溶液中反应生成。通过二次离子质谱、红外光谱和核磁共振波谱技术对这些配合物进行了表征。
• [EN] DRUG DELIVERY COMPOSITIONS AND METHODS<br/>[FR] COMPOSITIONS ET MÉTHODES POUR LA DISTRIBUTION DE MÉDICAMENTS
  申请人：UNIV KANSAS

  公开号：WO2017120193A1

  公开（公告）日：2017-07-13

  One aspect of the present invention is directed to conjugates that comprise a linear polymer carrier, a linker and one or more drugs or imaging agents, as well as pharmaceutical compositions that include such conjugates. The drug may be a platinum-containing drug with a linker comprised of a modified amino acid. The conjugate may alternatively include a metal complexing ligand with a metal used for imaging or chemotherapeutic purposes. Another aspect of the invention is directed to formulations and processes for lyophilization of hyaluronan conjugates. Another aspect of the invention is directed to methods for treating and/or inhibiting cancer utilizing the conjugates and compositions described herein.

  本发明的一个方面涉及共轭物，其包括线性高分子载体、连接剂和一个或多个药物或成像剂，以及包括这种共轭物的药物组合物。药物可以是含铂药物，连接剂由修饰的氨基酸组成。共轭物也可以包括金属络合配体，金属用于成像或化疗目的。本发明的另一个方面涉及透明质酸共轭物的冻干制剂和制备方法。本发明的另一个方面涉及利用上述共轭物和组合物治疗和/或抑制癌症的方法。
• <i>trans</i>-Platinum(<scp>iv</scp>) pro-drugs that exhibit unusual resistance to reduction by endogenous reductants and blood serum but are rapidly activated inside cells:¹H NMR and XANES spectroscopy study
  作者：Catherine K. J. Chen、Peter Kappen、Dan Gibson、Trevor W. Hambley

  DOI：10.1039/d0dt01622e

  日期：——

  complexes that they do to cis-diam(m)ineplatinum complexes. The cis complexes exhibit resistance to reduction by L-ascorbate and human blood serum, but are readily reduced inside cancer cells. Studies of reduction monitored by 1H NMR revealed that oxidation of trans-diammineplatinum(II) complexes does not always result in significant stabilisation, but the complexes trans, trans, trans-[Pt(OAc)4(NH3)2]

  最近的结果证实，保护跨铂不受癌细胞通路反应的影响，从而大大增强了它们的活性，表明这种复合物的潜力比以前认为的要大。在这项研究中，我们研究了铂（IV）氧化态和四羧酸盐配位球的使用，以确定这些特征是否能赋予反式-diammineplatinum络合物与顺式-dimm（m）ineplatinum络合物相同的稳定性。所述顺式配合物表现出对通过还原性大号-ascorbate和人血清，但癌细胞内部容易降低。减量研究由1监控1 H NMR表明，反式-diammineplatinum（II）配合物的氧化并不总是导致稳定，但是该配合物反式，反式，反式-[Pt（OAc）4（NH 3）2 ]（OAc =乙酸盐）和反式，反式，反式-[Pt（OPr）2（OAc）2（NH 3）2 ]（OPr =丙酸酯）在十倍过量的L-存在下分别表现出33 h和5.9天的二级半衰期。抗坏血酸。血液模型减少的XANES光谱研究表明，反式
• The hydrolysis products of cis-dichlorodiammineplatinum(II) 2. The kinetics of formation and anation of the cis-diamminedi(aqua)platinum(II) cation
  作者：Sian E. Miller、Donald A. House

  DOI：10.1016/s0020-1693(00)80810-5

  日期：1989.12

  cis-PtCl(OH)(NH3)2 (k2OH, s−1) generated by basification of cis-PtCl(NH3)2(OH2)+ is similar to k12OH, with k2OH = 1.43 × 10−5 s−1, ΔH‡ = 84.3 and ΔS‡ = −55 at 25 °C (μ = 0.1 M). Acidification of cis-Pt(OH)2(NH3)2 (generated from cis-PtCl2(NH3)2 in 0.01 M NaOH) rapidly forms cis-Pt(NH3)2(OH2)2+ and this, in turn is slowly anated by the background chloride ion to give an equilibrium cis-PtCl(NH3)2(OH2)+, cis-Pt(NH3)2(OH2)22+

  在碱性溶液（[OH - ]⩾0.01 M），顺式-PtCl 2（NH 3）2经受的水解均为氯配体，得到顺式-Pt（OH）2（NH 3）2作为稳定的最终产物。已经在35°C的温度范围内，在含有NaClO 4（μ= 0.01-1.0 M）或NaCl（0.1-1.0 M）的NaOH水溶液（0.01–1.0 M）中用分光光度法研究了该反应的速率。反应速率几乎不受[OH的- ]，离子强度和加入的氯离子，并在25°C（μ= 0.1M，次氯酸钠4），ķ 12 OH = 1.90×10-5 s -1，ΔH ‡＝ 84.4kJ mol -1，ΔS ‡＝ -52JK -1 mol -1。顺式-PtCl（NH 3）2（OH 2）+碱化生成的顺式-PtCl（OH）（NH 3）2（k 2 OH，s -1）中氯配体的损失速率与k相似12 OH，k 2 OH = 1.43×10 -5 s -1，ΔH ‡ = 84.3，ΔS
• Gmelin Handbuch der Anorganischen Chemie, Gmelin Handbook: Pt: MVol.D, 87, page 207 - 209
  作者：

  DOI：——

  日期：——