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Title

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

AuthorsCerrada, Elena ; Laguna, Mariano ; Mendía, Aránzazu
Issue Date2013
PublisherAmerican Chemical Society
CitationInorganic Chemistry 52(11): 6635-6647 (2013)
AbstractA 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 [Pd 2Cl2(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. © 2013 American Chemical Society.
URIhttp://hdl.handle.net/10261/111464
DOI10.1021/ic4006746
Identifiersdoi: 10.1021/ic4006746
issn: 0020-1669
e-issn: 1520-510X
Appears in Collections:(ISQCH) Artículos
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