期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 105, 期 6, 页码 793-799出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2011.03.001
关键词
Trans-Pt complexes; Histone deactylase inhibitor; Valproic acid; Cytotoxicity; Mutagenicity
资金
- Science Foundation Ireland [07/RFP/CHEF570, 08/RFP/CHE1675]
- European Social Fund
- Programme for Research in Third Level Institutions (PRTLI)
- Science Foundation Ireland (SFI) [08/RFP/CHE1675, 07/RFP/CHEF570] Funding Source: Science Foundation Ireland (SFI)
The first examples of Pt complexes of the well known anti-epilepsy drug and histone deacetylase inhibitor, valproic acid (VPA), are reported. Reaction of the Pt(II) am(m)ine precursors trans-(PtCl2(NH3)(py)] and trans-[PtCl2(py)(2)] with silver nitrate and subsequently sodium valproate gave trans-[Pt(VPA(-1H))(2)(NH3)(py)] and trans-[Pt(VPA(-1H))(2)(py)(2)], respectively. The valproato ligands in both complexes are bound to the Pt(II) centres via the carboxylato functionality and in a monodentate manner. The X-ray crystal structure of trans-[Pt(VPA(-1H))(2)(NH3)(py)] is described. Replacement of the dichlorido ligands in trans-[PtCl2(py)(2)] and trans-[PtCl2(NH3)(py)] by valproato ligands (VPA(-1H)) to yield trans-[Pt(VPA(-1H))(2)(py)(2)] and trans-[Pt(VPA(-1H))(2)(NH3)(py)(2)] respectively, significantly enhanced cytotoxicity against A2780 (parental) and A2780 cisR (cisplatin resistant) ovarian cancer cells. The mutagenicity of trans-[Pt(VPA(-1H))(2)(NH3)(py)] and trans-[Pt(VPA(-1H))(2)(py)(2)] was determined using the Ames test and is also reported. (C) 2011 Elsevier Inc. All rights reserved.
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