Medina Rosa M, Rodríguez Jorge, Quiroga Adoración G, Ramos-Lima Francisco J, Moneo Victoria, Carnero Amancio, Navarro-Ranninger Carmen, Macazaga María J
Departamento de Química Inorgánica, Universidad Autónoma de Madrid, ES-28049 Madrid, (phone: +34-91-4973870; fax: +34-91-4974833).
Present address: School of Chemistry, Bristol University.
Chem Biodivers. 2008 Oct;5(10):2090-2100. doi: 10.1002/cbdv.200890190.
trans-Pt(II) Complexes with aliphatic amines and planar amines such as (hydroxymethyl)pyridines, and pyridine-3- and pyridine-4-carboxylic acids were synthesized and screened for their potential cytotoxic activity in different cancer cell lines used at the NCI for in vitro screens, i.e., MCF7, NCIH460, and SF268. The complexes studied were designed to differ in geometrical parameters such as the position of the phenyl-group substituents and the nature of the substituents themselves for gathering information about the structure-activity relationships in the trans-complexes. The variation of the substituents turns to be crucial for their biological activity, as both pyridine-3- and pyridine-4-carboxylic acids in trans-position to both amine and isopropylamine ligands provided complexes which displayed no specificity toward any type of cell tested, while (hydroxymethyl)pyridine in trans-position to isopropylamine ligands led to complexes that were clearly more effective against the cell lines tested.
合成了与脂肪族胺以及平面胺（如（羟甲基）吡啶）、吡啶 - 3 - 羧酸和吡啶 - 4 - 羧酸形成的反式铂（II）配合物，并在国立癌症研究所（NCI）用于体外筛选的不同癌细胞系（即MCF7、NCIH460和SF268）中对其潜在的细胞毒性活性进行了筛选。所研究的配合物在几何参数上有所不同，例如苯基取代基的位置以及取代基本身的性质，以便收集有关反式配合物结构 - 活性关系的信息。取代基的变化对其生物活性至关重要，因为与胺和异丙胺配体均处于反位的吡啶 - 3 - 羧酸和吡啶 - 4 - 羧酸所形成的配合物对所测试的任何类型细胞均无特异性，而与异丙胺配体处于反位的（羟甲基）吡啶所形成的配合物对所测试的细胞系明显更有效。
