A new compound [Cu(AFO)2(N3)2](DMF)(H2O)(AFO=4,5-diazafluorene-9-one)was synthesized.Its structure was determined by single X-ray diffraction.The crystal belongs to monoclinic system,space group C2/c.The cry...A new compound [Cu(AFO)2(N3)2](DMF)(H2O)(AFO=4,5-diazafluorene-9-one)was synthesized.Its structure was determined by single X-ray diffraction.The crystal belongs to monoclinic system,space group C2/c.The crystallographic data,were determined a=1.2609(2)nm,b=0.8000(1)nm,c=2.6220(4)nm,β=109.964(6)°,V=2.4859(6)nm3,Z=4,F(000)=1236,Mr=603.07,Dc=1.611 Mg/m3,μ=0.937 nm-1,R1=0.0561,and wR2=0.1290.In the crystal Cu(II) atom is coordinated with four nitrogen from two AFO ligands and two nitrogen atoms from two azide ions to form an elonged-octahedron geometry.展开更多
目的设计合成两种不同结构的平面正方形铂(II)配合物,探讨其抗肿瘤活性及机制。方法通过噻唑蓝(MTT)法对配合物4和配合物5的体外细胞毒性进行测试;利用ICP-MS(Inductively coupled plasma mass spectrometry)方法对配合物在细胞内分布...目的设计合成两种不同结构的平面正方形铂(II)配合物,探讨其抗肿瘤活性及机制。方法通过噻唑蓝(MTT)法对配合物4和配合物5的体外细胞毒性进行测试;利用ICP-MS(Inductively coupled plasma mass spectrometry)方法对配合物在细胞内分布进行分析;通过蛋白免疫印迹的方法检测配合物影响肿瘤细胞核内γH2AX抗体的变化;使用Caspase-Glo®试剂盒检测配合物损伤细胞的形式,并且通过扫描电镜拍摄观察细胞损伤的形式。结果配合物4和配合物5的细胞半数抑制浓度(IC_(50))值均明显低于顺铂,在HeLa细胞中分别为(4.4±0.2)和(8.2±0.2)μmol·L^(-1),配合物4细胞毒性是顺铂的约4倍。配合物4和配合物5能定位在细胞核内,以细胞凋亡方式损伤细胞核DNA,具有较强的体外抗肿瘤活性。结论氮杂环卡宾铂(II)配合物具有良好的细胞毒性,通过诱导DNA损伤杀伤肿瘤细胞。展开更多
文摘A new compound [Cu(AFO)2(N3)2](DMF)(H2O)(AFO=4,5-diazafluorene-9-one)was synthesized.Its structure was determined by single X-ray diffraction.The crystal belongs to monoclinic system,space group C2/c.The crystallographic data,were determined a=1.2609(2)nm,b=0.8000(1)nm,c=2.6220(4)nm,β=109.964(6)°,V=2.4859(6)nm3,Z=4,F(000)=1236,Mr=603.07,Dc=1.611 Mg/m3,μ=0.937 nm-1,R1=0.0561,and wR2=0.1290.In the crystal Cu(II) atom is coordinated with four nitrogen from two AFO ligands and two nitrogen atoms from two azide ions to form an elonged-octahedron geometry.
文摘目的设计合成两种不同结构的平面正方形铂(II)配合物,探讨其抗肿瘤活性及机制。方法通过噻唑蓝(MTT)法对配合物4和配合物5的体外细胞毒性进行测试;利用ICP-MS(Inductively coupled plasma mass spectrometry)方法对配合物在细胞内分布进行分析;通过蛋白免疫印迹的方法检测配合物影响肿瘤细胞核内γH2AX抗体的变化;使用Caspase-Glo®试剂盒检测配合物损伤细胞的形式,并且通过扫描电镜拍摄观察细胞损伤的形式。结果配合物4和配合物5的细胞半数抑制浓度(IC_(50))值均明显低于顺铂,在HeLa细胞中分别为(4.4±0.2)和(8.2±0.2)μmol·L^(-1),配合物4细胞毒性是顺铂的约4倍。配合物4和配合物5能定位在细胞核内,以细胞凋亡方式损伤细胞核DNA,具有较强的体外抗肿瘤活性。结论氮杂环卡宾铂(II)配合物具有良好的细胞毒性,通过诱导DNA损伤杀伤肿瘤细胞。