| 氨·环己胺·羧酸根合铂(Ⅱ)类配合物的合成、抗肿瘤活性和与DNA的键合水平(英文) |
| Synthesis, Cytotoxicity and DNA-Binding Levels of Amminecyclohexy/Aminecarboxy/Platinum(Ⅱ) Complexes |
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| 摘要: 本工作设计合成了6种新型氨·环己胺·羧酸根合铂(Ⅱ)类配合物[Pt(NH3)((?)-NH2)X2](a～f){其中，X=CH3COO-(乙酸根)，CH2ClCOO-(氯乙酸根)，C6H5-COO-(苯甲酸根)，p-CH3O-C6 |
| 关键词: 混胺铂(Ⅱ)配合物 抗肿瘤活性 经典构效关系 细胞周期 Pt-DNA键合 |
| 基金项目: |
| Abstract: Six new amminecyclohexy/aminecarboxy/platinum(Ⅱ) complexes with carboxylates (a～f) have been synthesized and characterized by elemental analysis, conductivity, IR, UV, and 1H NMR spectra techniques. The cytotoxicity of the complexes was tested by MTT assay. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP-MS. The results show that complexes (c), (d), (e) and (f) have excellent cytotoxicity against EJ and HL-60 and complexes (c), (d) and (e) demonstrate cytotoxicity superior to that of the clinically established cisplatin. Complexes (a～f) have poor cytotoxicity against HCT-8, MCF-7 and BGC-823 than that of cisplatin. The complexes (a～f) induce a concentration-dependent accumulation of HL-60 and EJ cells in the G2 / M phase of the cell cycle as cisplatin. The levels of total platinum bound to DNA in HL-60 and EJ cells decrease in the sequence: c > d > e > cisplatin > f > a > b under the same experimental conditions. |
| Keywords: amine platinum(Ⅱ) complexes antitumor activity classical structure-activity relationships cell cycle Pt-DNA binding |
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| 张金超,申勇,杨梦苏.氨·环己胺·羧酸根合铂(Ⅱ)类配合物的合成、抗肿瘤活性和与DNA的键合水平(英文)[J].无机化学学报,2006,22(5):823-831. |
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