以3-吲哚丙酸为原料,经环化、N-甲基化、Claisen-Schmidt缩合和环加成反应合成了新型氨基嘧啶环戊并[b]吲哚衍生物,其结构经1 H NMR、13 C NMR及HR-MS(ESI)表征。采用细胞增殖抑制实验法(MTT法)测定了6a^6j对人肝癌(HepG-2)、人子宫颈癌...以3-吲哚丙酸为原料,经环化、N-甲基化、Claisen-Schmidt缩合和环加成反应合成了新型氨基嘧啶环戊并[b]吲哚衍生物,其结构经1 H NMR、13 C NMR及HR-MS(ESI)表征。采用细胞增殖抑制实验法(MTT法)测定了6a^6j对人肝癌(HepG-2)、人子宫颈癌(Hela)和人鼻咽癌(CNE-1)瘤株的体外抑制活性。结果表明:6b的抑制活性最好,IC 50值分别为大于50μmol/L(HepG-2)、15.2μmol/L(Hela)和14.8μmol/L(CNE-1)。展开更多
A novel potential tridentate Schiff base was prepared by condensing equimolar quantities of 2-hydroxyacetophenone and 2-aminopyrimidine in methanol. This ligand was versatile in forming a series of complexes with lant...A novel potential tridentate Schiff base was prepared by condensing equimolar quantities of 2-hydroxyacetophenone and 2-aminopyrimidine in methanol. This ligand was versatile in forming a series of complexes with lanthanide ions such as La（III）, Pr（III）, Nd（III）, Sm（III）, Gd（III）, Dy（III） and Yb（III）. The ligand and the metal complexes were characterized through elemental analysis, molar conductance, UV-Visible, IR, 1H NMR, and mass spectral studies. The spectral studies indicated that the ligand was coordinated to the metal ion in neutral tridentate fashion through the azomethine nitrogen, one of the nitrogen atoms in the pyrimidine ring and the phenolic oxygen without deprotonation. Thermal decomposition and luminescence property of lanthanum（III） complex were also examined. The X-ray diffraction patterns showed the crystalline nature of the ligand and its lanthanum（III） complex. The DNA cleavage studies of the ligand and the metal complexes were carried out and it was observed that the lanthanum（III） and neo-dymium（III） complexes cleaved the pUC19 DNA effectively. The ligand and the metal complexes were screened for their antibacte-rial activities. The metal complexes were found to be more potent bactericides than the ligand.展开更多
文摘以3-吲哚丙酸为原料,经环化、N-甲基化、Claisen-Schmidt缩合和环加成反应合成了新型氨基嘧啶环戊并[b]吲哚衍生物,其结构经1 H NMR、13 C NMR及HR-MS(ESI)表征。采用细胞增殖抑制实验法(MTT法)测定了6a^6j对人肝癌(HepG-2)、人子宫颈癌(Hela)和人鼻咽癌(CNE-1)瘤株的体外抑制活性。结果表明:6b的抑制活性最好,IC 50值分别为大于50μmol/L(HepG-2)、15.2μmol/L(Hela)和14.8μmol/L(CNE-1)。
文摘A novel potential tridentate Schiff base was prepared by condensing equimolar quantities of 2-hydroxyacetophenone and 2-aminopyrimidine in methanol. This ligand was versatile in forming a series of complexes with lanthanide ions such as La（III）, Pr（III）, Nd（III）, Sm（III）, Gd（III）, Dy（III） and Yb（III）. The ligand and the metal complexes were characterized through elemental analysis, molar conductance, UV-Visible, IR, 1H NMR, and mass spectral studies. The spectral studies indicated that the ligand was coordinated to the metal ion in neutral tridentate fashion through the azomethine nitrogen, one of the nitrogen atoms in the pyrimidine ring and the phenolic oxygen without deprotonation. Thermal decomposition and luminescence property of lanthanum（III） complex were also examined. The X-ray diffraction patterns showed the crystalline nature of the ligand and its lanthanum（III） complex. The DNA cleavage studies of the ligand and the metal complexes were carried out and it was observed that the lanthanum（III） and neo-dymium（III） complexes cleaved the pUC19 DNA effectively. The ligand and the metal complexes were screened for their antibacte-rial activities. The metal complexes were found to be more potent bactericides than the ligand.
