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Title: Exploring the scope of [Pt2(4-FC6H4)4(μ-SEt2)2] as a precursor for new organometallic platinum(II) and platinum(IV) antitumor agents
Author: Escolà Jané, Anna
Crespo Vicente, Margarita Ma.
Quirante Serrano, Josefina
Cortés Giràldez, Roldàn
Jayaraman, A.
Badía Palacín, Josefa
Baldomà Llavinés, Laura
Calvet Pallàs, Maria Teresa
Font Bardia, Ma. Mercedes
Cascante i Serratosa, Marta
Keywords: Química organometàl·lica
Medicaments antineoplàstics
Estructura molecular
Organometallic chemistry
Antineoplastic agents
Molecular structure
Issue Date: 2014
Publisher: American Chemical Society
Abstract: The new compound [Pt2(4-FC6H4)4(μ-SEt2)2] (A) was prepared and fully characterized. The reactions of compound A with ligands ArCH=NCH2CH2NMe2 (Ar = 2-BrC6H4, 1a; 2,6-Cl2C6H3, 1b; 4-ClC6H4, 1c; 2-Cl,6-FC6H3, 1d) were studied under different conditions and produced platinum(II) compounds [Pt(4-FC6H4)2(ArCH=NCH2CH2NMe2)] (2b−2d), containing a bidentate [N,N′] ligand, as well as cyclometalated platinum(IV) or platinum(II) compounds such as [PtBr(4-FC6H4)2(C6H4CH=NCH2CH2NMe2)] (4a) or [PtCl{(3-FC6H3)(2-XC6H3)CH=NCH2CH2NMe2}] (5b: X = Cl; 5d: X = F), containing a tridentate [C,N,N′] ligand and either a five (4a) or a seven (5b, 5d) membered metallacycle. These compounds exhibit a great antiproliferative activity against non-small lung cancer cells (A549), and the best result was obtained for compound 2c (IC50 = 0.3 ± 0.1 μM). While compounds 5 alter the mobility of plasmid DNA in a similar way to cisplatin, compound 4 was less efficient in removing the supercoils from DNA. In spite of the very low IC50 value obtained for compound 2c, this compound does not interact with DNA, and it is neither an intercalator nor a topoisomerase I inhibitor.
Note: Versió postprint del document publicat a:
It is part of: Organometallics, 2014, vol. 33, num. 7, p. 1740-1750
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ISSN: 0276-7333
Appears in Collections:Articles publicats en revistes (Mineralogia, Petrologia i Geologia Aplicada)

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