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http://hdl.handle.net/2445/163390
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DC Field | Value | Language |
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dc.contributor.author | Bauer, Emma | - |
dc.contributor.author | Domingo, Xavier | - |
dc.contributor.author | Balcells, C. | - |
dc.contributor.author | Polat, Ibrahim H. | - |
dc.contributor.author | Crespo Vicente, Margarita Ma. | - |
dc.contributor.author | Quirante Serrano, Josefina | - |
dc.contributor.author | Badía Palacín, Josefa | - |
dc.contributor.author | Baldomà Llavinés, Laura | - |
dc.contributor.author | Font Bardia, Ma. Mercedes | - |
dc.contributor.author | Cascante i Serratosa, Marta | - |
dc.date.accessioned | 2020-05-31T14:42:16Z | - |
dc.date.available | 2020-05-31T14:42:16Z | - |
dc.date.issued | 2017-11-21 | - |
dc.identifier.issn | 1477-9226 | - |
dc.identifier.uri | http://hdl.handle.net/2445/163390 | - |
dc.description.abstract | The synthesis of six novel cyclometallated platinum(IV) iodido complexes is accomplished by intermolecular oxidative addition of methyl iodide (compounds 2a-2c) or iodine (compounds 3a-3c) upon cyclometallated platinum(II) compounds [PtX{(CH3)(2)N(CH2)(3)NCH(4-ClC6H3)}] (1a-1c: X = Cl, CH3 or I). The X-ray molecular structures of platinum(II) compound 1c and platinum(IV) compounds 3b and 3a' (an isomer of 3a) are reported. The cytotoxic activity against a panel of human adenocarcinoma cell lines (A-549 lung, MDA-MB-231 and MCF-7 breast, and HCT-116 colon), DNA interaction, topoisomerase I, II alpha, and cathepsin B inhibition, and cell cycle arrest, apoptosis and ROS generation of the investigated complexes are presented. Remarkable antiproliferative activity was observed for most of the synthesized cycloplatinated compounds (series 1-3) in all the selected carcinoma cell lines. The best inhibition was provided for the octahedral platinum(IV) compounds 2a-2c exhibiting a methyl and an iodido axial ligand. Preliminary biological results point to a different mechanism of action for the investigated compounds. Cyclometallated platinum(II) compounds 1a-1c modify the DNA migration as cisplatin. In contrast, cyclometallated platinum(IV) compounds 2a-2c and 3a-3c did not modify the DNA tertiary structure neither in the absence nor in the presence of ascorbic acid, which made them incapable of reducing platinum(IV) compounds 2b and 2c in a buffered aqueous medium (pH 7.40) according to H-1 NMR experiments. Remarkable topoisomerase II alpha inhibitory activity is reported for platinum(IV) complexes 2b and 3a and in addition, for the last one, a moderate cathepsin B inhibition is reported. Cell cycle arrest (decrease in G0/G1 and G2 phases and arrest in the S phase), induction of apoptosis and ROS generation are related to the antiproliferative activity of some representative octahedral cyclometallated platinum(IV) compounds (2b and 2c). | - |
dc.format.extent | 45 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Royal Society of Chemistry | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1039/c7dt03448b | - |
dc.relation.ispartof | Dalton Transactions, 2017, vol. 46, num. 43, p. 14973-14987 | - |
dc.relation.uri | https://doi.org/10.1039/c7dt03448b | - |
dc.rights | (c) Bauer, Emma et al., 2017 | - |
dc.source | Articles publicats en revistes (Mineralogia, Petrologia i Geologia Aplicada) | - |
dc.subject.classification | Platí | - |
dc.subject.classification | Metalls | - |
dc.subject.other | Platinum | - |
dc.subject.other | Metals | - |
dc.title | Synthesis, characterization and biological activity of new cyclometallated platinum(IV) iodido complexes | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 677619 | - |
dc.date.updated | 2020-05-31T14:42:17Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Mineralogia, Petrologia i Geologia Aplicada) |
Files in This Item:
File | Description | Size | Format | |
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677619.pdf | 1.98 MB | Adobe PDF | View/Open |
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