β-二酮配体离去基团的顺二氨二氯合铂（II）配合物的体外抗癌活性。
In vitro anticancer activity of cis-diammineplatinum(II) complexes with β-diketonate leaving group ligands.
机构信息
Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.
出版信息
J Med Chem. 2012 Jun 14;55(11):5326-36. doi: 10.1021/jm3002857. Epub 2012 May 18.
Abstract
Five cationic platinum(II) complexes of general formula, [Pt(NH(3))(2)(β-diketonate)]X are reported, where X is a noncoordinating anion and β-diketonate = acetylacetonate (acac), 1,1,1,-trifluoroacetylacetonate (tfac), benzoylacetonate (bzac), 4,4,4-trifluorobenzoylacetonate (tfbz), or dibenzoylmethide (dbm), corresponding, respectively, to complexes 1-5. The log P values and the stabilities of 1-5 in aqueous solution were evaluated. The phenyl ring substituents of 3-5 increase the lipophilicity of the resulting complexes, whereas the trifluoromethyl groups of 2 and 4 decrease the stability of the complexes in aqueous solution. The uptake of 1-5 in HeLa cells increases as the lipophilicity of the investigated complex increases. Cancer cell cytotoxicity studies indicate that 1 and 3 are the least active complexes whereas 2, 4, and 5 are comparable in activity to cisplatin.
摘要
报道了 5 种具有通式[Pt(NH3)2(β-二酮)]X 的阳离子铂(II)配合物，其中 X 为非配位阴离子，β-二酮=乙酰丙酮（acac）、1,1,1-三氟乙酰丙酮（tfac）、苯甲酰丙酮（bzac）、4,4,4-三氟苯甲酰丙酮（tfbz）或二苯甲酮（dbm），分别对应于配合物 1-5。评估了 1-5 在水溶液中的 log P 值和稳定性。3-5 的苯环取代基增加了所得配合物的亲脂性，而 2 和 4 的三氟甲基降低了配合物在水溶液中的稳定性。HeLa 细胞对 1-5 的摄取随着所研究配合物亲脂性的增加而增加。癌细胞细胞毒性研究表明，1 和 3 是最不活跃的配合物，而 2、4 和 5 的活性与顺铂相当。
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