New bioactive 2,6-diacetylpyridine bis(p-chlorophenylthiosemicarbazone) ligand and its Pd(II) and Pt(II) complexes: Synthesis, characterization, cytotoxic activity and DNA binding ability
Entity
UAM. Departamento de Química InorgánicaPublisher
Elsevier Inc.Date
2014-05-09Citation
10.1016/j.jinorgbio.2014.04.017
Journal of Inorganic Biochemistry 138 (2014): 16-23
ISSN
0162-0134 (print); 1873-3344 (online)DOI
10.1016/j.jinorgbio.2014.04.017Funded by
We are grateful to Ministerio de Economía y Competitividad, Instituto de Salud Carlos III of Spain (PI1100659) for financial supportEditor's Version
http://dx.doi.org/10.1016/j.jinorgbio.2014.04.017Subjects
2,6-Diacetylpyridine; Antitumor activity; Asymmetric coordination; Palladium and platinum complexes; Thiosemicarbazone; QuímicaNote
NOTICE: this is the author’s version of a work that was accepted for publication in Journal of Inorganic Biochemistry. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Journal of Inorganic Biochemistry 138 (2014): 16-23 DOI http://dx.doi.org/10.1016/j.jinorgbio.2014.04.017Rights
© 2014 Elsevier Inc. All rights reservedEsta obra está bajo una licencia de Creative Commons Reconocimiento-NoComercial-SinObraDerivada 4.0 Internacional.
Abstract
Preparation and characterization of 2,6-diacetylpyridine bis(4N-p-chlorophenylthiosemicarbazone) ligand, H2L, and its palladium(II) and platinum(II) complexes [PdL] and [PtL], is described. The molecular structure of the two new complexes has been determined by single crystal X-ray diffraction. The ligand acts as dianionic tetradentate donor coordinating to the metal center in a square planar geometry through the pyridine nitrogen atom and the azomethine nitrogen and thione sulfur atoms from one thiosemicarbazone arm, the fourth coordination position is occupied by the hydrazine nitrogen atom of the other arm. New free ligand and its metal complexes have been evaluated for antiproliferative activity in vitro against NCI-H460, T-47D, A2780 and A2780cisR human cancer cell lines. The cytotoxicity data suggest that these compounds may be endowed with important antitumor properties, especially H2L and [PtL] since they are capable of not only circumvent cisplatin resistance in A2780cisR cells but also exhibit high antiproliferative activity in breast cancer T-47D cells. The interaction of H2L with calf thymus DNA was also investigated and its binding constant (Kb) determined
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Google Scholar:Matesanz García, Ana Isabel
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Hernández, Carolina
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Souza, Pilar
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