Novel bis(thiosemicarbazones) of the 3,5-diacetyl-1,2,4-triazol series and their platinum(ii) complexes: chemistry, antiproliferative activity and preliminary nephrotoxicity studies
Entity
UAM. Departamento de Química InorgánicaPublisher
Royal Society of ChemistryDate
2011-06-07Citation
10.1039/c1dt10212e
Dalton Transactions 40.21 (2011): 5738-5745
ISSN
1477-9226 (print); 1477-9234 (on line)DOI
10.1039/c1dt10212eFunded by
We are grateful to Ministerio de Ciencia e Innovación, Instituto de Salud Carlos III (PI080525), Universidad Autónoma de Madrid and Comunidad de Madrid (CCG08-UAM/SAL-4000) of Spain for financial supportEditor's Version
http://dx.doi.org/10.1039/c1dt10212eSubjects
Platinum compounds; Human Cancer Cells; QuímicaNote
Dalton Transactions 40.21 (2011): 5738-5745. Reproduced by permission of The Royal Society of ChemistryRights
© The Royal Society of Chemistry 2011Abstract
The preparation and characterization of three novel 4N- monosubstituted bis(thiosemicarbazone) ligands of 3,5-diacetyl-1,2,4-triazol series and their dinuclear platinum complexes are described. The crystal and molecular structure of the [Pt(μ-H3L3)]2 complex derived of 3,5-diacetyl-1,2,4-triazol bis(4N-p- tolylthiosemicarbazone), H5L3, has been resolved by single crystal X-ray diffraction. The ligands coordinate, in an asymmetric dideprotonate form, to the platinum ions in a tridentate fashion (NNS) and S-bridging bonding modes. Thus the molecular units of the platinum complexes are stacked as dimers. The new compounds synthesized have been evaluated for antiproliferative activity in vitro against NCI-H460, A2780 and A2780cisR human cancer cell lines. The cytotoxicity data suggest that these compounds may be endowed with important antitumour properties since are capable of not only circumventing cisplatin resistance in A2780cisR cells but also exhibit high antiproliferative activity in human non-small cell lung cancer NCI-H460 cells. The interactions of these compounds with calf thymus DNA was investigated by UV-vis absorption and a nephrotoxic study, in LLC-PK1 cells, has also been carried out
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Google Scholar:Matesanz García, Ana Isabel
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Hernández, Carolina
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Rodríguez, Ana
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Souza, Pilar
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