Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2017-08-08 , DOI: 10.1016/j.jinorgbio.2017.07.035 Katia G. Samper , Sierra C. Marker , Pau Bayón , Samantha N. MacMillan , Ivan Keresztes , Òscar Palacios , Justin J. Wilson
The syntheses of three platinum(II) complexes bearing sulfonamide-((E)-2-(4-methylphenylsulfonamido)-2′,6′-difluoroazobenzene, HL1) and hydroxy-azo-2,6-difluorobenzene ((E)-2-((2,6-difluorophenyl)diazenyl)phenol, HL2) bidentate ligands is described. These complexes, [Pt(L1)(DMSO)Cl] (1), [Pt(L2)(DMSO)Cl] (2), and [Pt(L2)2] (3), were characterized by multinuclear NMR spectroscopy, mass spectrometry, and X-ray crystallography. Despite bearing azobenzene functional groups, none of the three complexes undergo photoisomerization. The anticancer activities of these complexes were evaluated in wild-type (A2780) and cisplatin-resistant (A2780CP70) ovarian cancer cells. All three complexes exhibited IC50 values below 10 μM and displayed similar activity in both A2780 and A2780CP70 cell lines, indicating that they are not cross-resistant with cisplatin. The DNA-binding properties of 1–3 were investigated by circular dichroism spectroscopy and by agarose gel electrophoresis. Both studies suggest that 1 and 2 form monofunctional DNA adducts.
中文翻译:
重印“羟基和磺酰胺-偶氮苯铂(II)配合物在顺铂耐药卵巢癌细胞中的抗癌活性”
带有磺酰胺-((E)-2-(4-甲基苯基磺酰胺基)-2',6'-二氟偶氮苯HL1和羟基-偶氮-2,6-二氟苯((E)-描述了2-((2,6-二氟苯基)二氮烯基)苯酚,HL2)双齿配体。这些络合物[Pt(L1)(DMSO)Cl](1),[Pt(L2)(DMSO)Cl](2)和[Pt(L2)2 ](3用多核NMR光谱,质谱和X射线晶体学进行表征。尽管带有偶氮苯官能团,这三种络合物均未进行光异构化。在野生型(A2780)和顺铂耐药(A2780CP70)卵巢癌细胞中评估了这些复合物的抗癌活性。这三种复合物在A2780和A2780CP70细胞系中均表现出低于10μM的IC 50值,并显示出相似的活性,表明它们与顺铂没有交叉耐药性。的DNA结合性质1 - 3通过圆二色光谱,并通过琼脂糖凝胶电泳进行了调查。两项研究均表明1和2 形成单功能DNA加合物。