Miernicka Magdalena, Szulawska Agata, Czyz Malgorzata, Lorenz Ingo-Peter, Mayer Peter, Karwowski Boleslaw, Budzisz Elzbieta
Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland.
J Inorg Biochem. 2008 Feb;102(2):157-65. doi: 10.1016/j.jinorgbio.2007.07.040. Epub 2007 Aug 10.
The new pyrazole ligand 5-(2-hydroxyphenyl)-3-methyl-1-(2-pyridylo)-1H-pyrazole-4-carboxylic acid methyl ester (2) and the corresponding Pt(II), Pd(II) and Cu(II) complexes 3-5 have been synthesized as potential anticancer compounds, and characterized using IR, and (1)H NMR as well as mass spectrometry. The 3-D structures of the Cu(II) complexes were determined by quantum mechanic calculation DFT methodology (density functional theory). The cytotoxicity assay of the ligand and complexes has been performed on leukemia cell lines. In general, the complexes showed lower cytotoxicity than cisplatin, and the Pt(II) and Cu(II) complexes were found to be more efficient in the induction of leukemia cell death than the Pd(II) complex. Our investigations indicate that the antiproliferating activity of the Pt(II) and Cu(II) complexes was partly due to the modulation of cellular differentiation.
新型吡唑配体5-(2-羟基苯基)-3-甲基-1-(2-吡啶基)-1H-吡唑-4-羧酸甲酯(2)以及相应的铂(II)、钯(II)和铜(II)配合物3-5已被合成为潜在的抗癌化合物，并通过红外光谱、核磁共振氢谱以及质谱进行了表征。铜(II)配合物的三维结构通过量子力学计算密度泛函理论(DFT)方法确定。已对白血病细胞系进行了配体和配合物的细胞毒性测定。总体而言，配合物的细胞毒性低于顺铂，并且发现铂(II)和铜(II)配合物在诱导白血病细胞死亡方面比钯(II)配合物更有效。我们的研究表明，铂(II)和铜(II)配合物的抗增殖活性部分归因于细胞分化的调节。
