Palladium(II) and platinum(II) bis(thiosemicarbazone) complexes of the 2,6-diacetylpyridine series with high cytotoxic activity in cisplatin resistant A2780cisR tumor cells and reduced toxicity

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• 作者：Ana I. Matesanz ; Iné ; s Leitao¹ ; Pilar Souza ; ^{pilar.souza@uam.es}
• 关键词：Antitumor activity ; Asymmetric N3S coordination ; 2 ; 6-Diacetylpyridine ; Palladium and platinum complexes ; Renal toxicity ; Thiosemicarbazone
• 刊名：Journal of Inorganic Biochemistry
• 出版年：2013
• 出版时间：August, 2013
• 年：2013
• 卷：125
• 期：Complete
• 页码：26-31
• 全文大小：459 K

文摘

Preparation and characterization of four novel 2,6-diacetylpyridine bis(⁴N-tolylthiosemicarbazonato) palladium(II) and platinum(II) complexes, [PdL^1-2] and [PtL^1-2], are described. All compounds have been characterized by elemental analysis and by IR and NMR spectroscopy, and the crystal and molecular structures of complexes [PdL²] and [PtL²] have been determined by a single crystal X-ray diffraction. The ligands act as dianionic tetradentate donors coordinating to the metal center in a square planar geometry through the N_pyridinic atom and the N_iminic and the S atoms from one thiosemicarbazone arm, the fourth coordination position is occupied by the N_hydrazinic of the other arm. The new compounds synthesized have been evaluated for antiproliferative activity in vitro against NCI-H460, HepG2, MCF-7, A2780 and A2780cisR human cancer cell lines. The cytotoxicity data suggest that [PdL¹], [PdL²] and [PtL²] may be endowed with important antitumor properties since they are capable of not only circumventing cisplatin resistance in A2780cisR cells but also exhibiting high antiproliferative activity in breast cancer MCF-7 cells. Subsequent toxicity study, in LLC-PK1 cells, has also been carried out and shows that none of these compounds are in vitro toxic in the tested concentration range.