Departamento de Química, Área de Química Inorgánica, Facultad de Ciencias, Universidad de Burgos, 09001 Burgos, Spain.
Inorg Chem. 2013 Jun 3;52(11):6635-47. doi: 10.1021/ic4006746. Epub 2013 May 21.
A series of PTA and DAPTA platinum(II) and palladium(II) thionate complexes of the type trans-[M(SN)2P2] were prepared from the reaction of cis-[MCl2P2] [M = Pt, Pd; P = PTA (1,3,5-triaza-7-phosphaadamantane), DAPTA (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane)] with the in situ generated sodium salts of the heterocyclic thiones S-m-methylpyrimidine-2-thione, S-4,6-dimethylpyrimidine-2-thione, S-4,6-dihydroxypyrimidine-2-thione, benzothiazole-2-thione, benzoxazole-2-thione, S-1,3,4,-thiadiazole-2-thione, S-4,5-H-thiazolan-2-thione, and S-pyrimidine-4(1H)-one-2-thione. The X-ray structures of six of the compounds confirm the trans disposition and, only in the case of [Pd2Cl2(S-pyrimidine-4(1H)-one-2-thionate)2(PTA)2], a dinuclear structure with a Pd-Pd distance of 3.0265(14)Å was observed. In vitro cytotoxicities against human ovarian cancer cell lines A2780 and A2780cisR were evaluated for ten complexes showing a high inhibition of cellular growth with a comparable inhibitory potency (IC50) against A2780 cells to that of cisplatin. Notably, the compounds also show significant (up to 7-fold higher) activity in cisplatin-resistant A2780cisR cell lines.
一系列 PTA 和 DAPTA 铂(II)和钯(II)硫代酸盐配合物，类型为 trans-[M(SN)2P2]，是由 cis-[MCl2P2] [M = Pt，Pd；P = PTA（1,3,5-三氮杂-7-磷杂金刚烷），DAPTA（3,7-二乙酰基-1,3,7-三氮杂-5-磷杂双环[3.3.1]壬烷）]与原位生成的杂环硫代物 S-甲基嘧啶-2-硫酮、S-4,6-二甲基嘧啶-2-硫酮、S-4,6-二羟基嘧啶-2-硫酮、苯并噻唑-2-硫酮、苯并恶唑-2-硫酮、S-1,3,4-噻二唑-2-硫酮、S-4,5-H-噻唑烷-2-硫酮和 S-嘧啶-4(1H)-酮-2-硫酮的钠盐反应制得。其中六个化合物的 X 射线结构证实了 trans 构型，并且仅在[Pd2Cl2(S-嘧啶-4(1H)-酮-2-硫代物)2(PTA)2]的情况下观察到具有 3.0265(14)Å Pd-Pd 距离的双核结构。对十种配合物对人卵巢癌细胞系 A2780 和 A2780cisR 的体外细胞毒性进行了评价，结果表明这些配合物对细胞生长有很高的抑制作用，对 A2780 细胞的抑制活性与顺铂相当。值得注意的是，这些化合物在顺铂耐药的 A2780cisR 细胞系中也具有显著（高达 7 倍）的活性。
