trans-Thionate Derivatives of Pt(II) and Pd(II) with Water-Soluble Phosphane PTA and DAPTA Ligands: Antiproliferative Activity against Human Ovarian Cancer Cell Lines

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• 作者：Elena Guerrero ; Susana Miranda ; Sebastian L眉ttenberg ; Nils Fr枚hlich ; Jan-Moritz Koenen ; Fabian Mohr ; Elena Cerrada ; Mariano Laguna ; Ar谩nzazu Mend铆a
• 刊名：Inorganic Chemistry
• 出版年：2013
• 出版时间：June 3, 2013
• 年：2013
• 卷：52
• 期：11
• 页码：6635-6647
• 全文大小：604K
• 年卷期：v.52,no.11(June 3, 2013)
• ISSN：1520-510X

文摘

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鈥揚d distance of 3.0265(14)脜 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.