Chemistry, antiproliferative activity and low nephrotoxicity of 3,5-diacetyl-1,2,4-triazol bis(4N-thiosemicarbazone) ligands and their platinum(ii) complexes
Metadatos
Title:
Chemistry, antiproliferative activity and low nephrotoxicity of 3,5-diacetyl-1,2,4-triazol bis(4N-thiosemicarbazone) ligands and their platinum(ii) complexes
Author:
Matesanz, Ana I.; Joie, Céline; Souza, Pilar
Entity:
UAM. Departamento de Química Inorgánica
Publisher:
Royal Society of Chemistry
Date:
2010-08-14
Citation:
10.1039/c003007d
Dalton Transactions 39.30 (2010): 7059-7065
ISSN:
1477-9226 (print); 1477-9234 (on line)
DOI:
10.1039/c003007d
Funded by:
We are grateful toMinisterio 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 support. C. J. also thanks Erasmus Programme for its Research Placement at Universidad Autónoma de Madrid
Editor's Version:
http://dx.doi.org/10.1039/c003007d
Subjects:
Chemistry; Química
Note:
Dalton Transactions 39.30 (2010): 7059-7065. Reproduced by permission of The Royal Society of Chemistry
Rights:
© The Royal Society of Chemistry 2010
Abstract:
The preparation and characterization of 3,5-diacetyl-1,2,4-triazol bis(4,4-dimethylthiosemicarbazone) ligand, H3L1, and its dinuclear platinum complex [Pt(μ-HL1)]2 is described. The crystal and molecular structure of the platinum complex 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 together with the analogous monosubstituted ligand 3,5-diacetyl-1,2,4-triazol bis(4-methylthiosemicarbazone) (H5L2) and its dinuclear platinum(ii) complex [Pt(μ-H3L2)]2 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 antitumor properties, especially H3L 1 and [Pt(μ-H3L2)]2 since they not only circumvent cisplatin resistance in A2780cisR cells but also exhibit high antiproliferative activity in human non-small cell lung cancer NCI-H460 cells. Subsequent nephrotoxic study, in LLC-PK1 cells, show that the four compounds investigated exhibit very low nephrotoxicity with respect to cisplatin
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