亲脂性铂（II）配合物的合成及其体外细胞毒性

Synthesis and in vitro cytotoxicity of lipophilic platinum(II) complexes.

作者信息

Kokotos G, Theodorou V, Constantinou-Kokotou V, Gibbons W A, Roussakis C

机构信息

Department of Chemistry, University of Athens, Greece.

出版信息

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1525-30. doi: 10.1016/s0960-894x(98)00256-x.

DOI:10.1016/s0960-894x(98)00256-x

PMID:9873383

Abstract

A number of lipophilic platinum(II) complexes of the general structures cis-[Pt(LA)2Cl2] and [Pt(LD)Cl2] were synthesised. Long chain amines (LA) and diamines (LD), prepared from lipidic amino acids, were used as ligands. The in vitro cytotoxicity of the complexes was evaluated against four cell lines (P388, NSCLC-N6, E39, M96). cis-Dichloro-bis(2-aminohexadecanol)platinum(II) was the most active against P388, NSCLC-N6 and E39 (IC50: 11 micrograms/ml, 25 micrograms/ml, 31 micrograms/ml), while dichloro(1,3-heptadecanediamine)platinum(II) presented the highest activity against M96 (IC50: 13 micrograms/ml).

摘要

合成了一系列具有顺式-[Pt(LA)2Cl2]和[Pt(LD)Cl2]一般结构的亲脂性铂(II)配合物。由脂族氨基酸制备的长链胺(LA)和二胺(LD)用作配体。评估了这些配合物对四种细胞系（P388、NSCLC-N6、E39、M96）的体外细胞毒性。顺式二氯双(2-氨基十六醇)铂(II)对P388、NSCLC-N6和E39的活性最高（IC50：11微克/毫升、25微克/毫升、31微克/毫升），而二氯(1,3-十七烷二胺)铂(II)对M96的活性最高（IC50：13微克/毫升）。