University of Vienna, Institute of Inorganic Chemistry, Waehringer Strasse 42, A-1090, Vienna, Austria.
Dalton Trans. 2011 Aug 28;40(32):8187-92. doi: 10.1039/c1dt10301f. Epub 2011 Jul 11.
(OC-6-43)-Dichlorido(N,N-dimethyl-ethane-1,2-diamine)dihydroxidoplatinum(IV) could selectively be mono-carboxylated with succinic anhydride based on the steric hindrance caused by the two methyl groups of the equatorial ligand. Subsequent esterification of the uncoordinated carboxylic acid with alcohols of different lengths (methanol, butanol, hexanol and octanol) afforded the corresponding esters. The synthesized complexes were characterized in detail by elemental analysis, ESI-MS, multinuclear ((1)H, (13)C, (15)N and (195)Pt) NMR spectroscopy and in two cases by X-ray crystallography. Cytotoxicity of novel platinum(IV) compounds was investigated in four human cancer cell lines (CH1, A549, SW480 and SK-OV-3). Remarkably, the most lipophilic complexes showed IC(50) values down to the low micromolar or even nanomolar range.
(OC-6-43)-二氯代（N，N-二甲基乙二胺）二羟基合铂（IV）可以根据配位体赤道位两个甲基的空间位阻选择性地与琥珀酸酐单羧化。随后，用不同长度的醇（甲醇、丁醇、己醇和辛醇）对未配位的羧酸进行酯化，得到相应的酯。通过元素分析、ESI-MS、多核（1H、13C、15N 和 195Pt）NMR 光谱以及两种情况下的 X 射线晶体学对合成的配合物进行了详细的表征。在四种人癌细胞系（CH1、A549、SW480 和 SK-OV-3）中研究了新型铂（IV）化合物的细胞毒性。值得注意的是，最亲脂性的配合物的 IC50 值低至低微摩尔甚至纳摩尔范围。
