Enhancement of aqueous solubility and stability employing a trans acetate axis in trans planar amine platinum compounds while maintaining the biological profile
Enhancement of aqueous solubility and stability employing a trans acetate axis in trans planar amine platinum compounds while maintaining the biological profile
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DOI：
10.1021/jm050539d
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发表时间：
2005-09-08
影响因子：
7.3
通讯作者：
Farrell, N
中科院分区：
文献类型：
--
作者：
Ma, ESF;Bates, WD;Farrell, N
一个通用的方法来溶解和可能的体内激活的transplatinum几何形状。介绍了新型水溶性细胞毒性反铂化合物的合成与表征。与母体二氯化物相比，在反式[Pt（OAc）（2）（L）（L ′）]中使用乙酸酯配体（和一般羧酸酯配体）导致显著增强的水溶性和化学稳定性。这些新化合物是第一个含有N2O2供体集的细胞毒性反铂化合物，类似于卡铂和奥沙利铂。
A general approach to solubilization and possible in vivo activation of the transplatinum geometry is presented. The synthesis and characterization of new water-soluble cytotoxic transplatinum compounds are described. Use of acetate ligands (and carboxylate ligands in general) in trans[Pt(OAc)(2)(L)(L')J results in significantly enhanced aqueous solubility and chemical stability in comparison to the parent dichlorides. The new compounds are the first cytotoxic transplatinum compounds containing an N2O2 donor set, similar to carboplatin and oxaliplatin.