Pastuszko Adam, Majchrzak Kinga, Czyz Malgorzata, Kupcewicz Bogumiła, Budzisz Elzbieta
Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland.
Department of Molecular Biology of Cancer, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
J Inorg Biochem. 2016 Jun;159:133-41. doi: 10.1016/j.jinorgbio.2016.02.020. Epub 2016 Feb 26.
A series of arene ruthenium(II) complexes with the general formula [(η(6)-arene)Ru(L)X2] (where arene=p-cymene, benzene, hexamethylbenzene or mesitylene, L=aminoflavone or aminochromone derivatives and X=Cl, I) were synthesized and characterized by elemental analysis, MS, IR and (1)H NMR spectroscopy. The stability of the selected complexes was assessed by UV-Vis spectroscopy in 24-hour period. The lipophilicity of the synthesized complexes was determined by the shake-flask method, and their cytotoxicity evaluated in vitro on patient-derived melanoma populations. The most active complexes against melanoma cells contain 7-aminoflavone and 6-aminoflavone as a ligand. The relationship between the cytotoxicity of all the obtained compounds and their logP values was determined and briefly analyzed with two different patterns observed.
合成了一系列通式为[(η(6)-芳烃)Ru(L)X2]的芳烃钌(II)配合物(其中芳烃 = 对异丙基苯、苯、六甲基苯或均三甲苯,L = 氨基黄酮或氨基色酮衍生物,X = Cl、I),并通过元素分析、质谱、红外光谱和(1)H核磁共振光谱对其进行了表征。通过紫外可见光谱在24小时内评估所选配合物的稳定性。采用摇瓶法测定合成配合物的亲脂性,并在体外对患者来源的黑色素瘤群体评估其细胞毒性。对黑色素瘤细胞活性最高的配合物含有7-氨基黄酮和6-氨基黄酮作为配体。确定了所有所得化合物的细胞毒性与其logP值之间的关系,并以观察到的两种不同模式进行了简要分析。