| 单功能铂配合物的合成表征、DNA结合和抗肿瘤活性(英文) |
| Synthesis, Characterization and DNA Binding Properties of Monofunctional Antitumor Pt(Ⅱ) Complexes |
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| 摘要: 本文合成了三种铂(Ⅱ)配合物PtLCl(HL1=2-(3′，5′-二甲基-吡唑-1′-基)-N-(2″-吡啶甲基)乙基胺；HL2=2-(3′，5′-二甲基-吡唑-1′-基)-N-(2″-吡啶乙基)乙基胺；HL3=2-(3′，5′-二甲基-吡唑-1′-基)-N-(喹啉-8″-基)乙基胺，通过元素分析和质谱进行结构表征。利用荧光和圆二色光谱研究了3种配合物与小牛胸腺DNA的相互作用，结果发现配体结构对配合物与DNA的作用方式及强度产生极大影响。PtL3Cl具有较大的共轭平面而易以嵌入模式与DNA结合，而PtL1Cl和PtL2Cl的空间位阻较小，易与DNA以共价模式结合。通过质谱跟踪发现，配合物PtL1Cl和PtL2Cl均能与5′-鸟苷酸(5′-GMP)发生共价结合，但是没有发现PtL3Cl与5′-GMP的加合物。3种配合物对人宫颈癌细胞的体外毒活性数据表明：PtL3Cl的细胞毒活性最强。 |
| 关键词: 吡唑铂配合物 DNA结合 细胞毒活性 |
| 基金项目: |
| Abstract: Three Pt(Ⅱ) complexes of pyrazolyl derivatives, PtLCl (HL1=2-(3′,5′-dimethyl-pyrazol-1′-yl)-N-(2″-pyridylmethyl)ethylamine; HL2=2-(3′,5′-dimethyl-pyrazol-1′-yl)-N-(2″-pyridylethyl)ethylamine and HL3=2-(3′,5′-dimethyl-pyrazol-1′-yl)-N-(quinolin-8″-yl)ethylamine have been synthesized and characterized. Fluorescence titration and circular dichroism analyses proved that coordination environment of the ligands remarkably influenced the interactions between their Pt(Ⅱ) complexes and DNA. The Pt(Ⅱ) complexes PtL1Cl and PtL2Cl could covalently combine to 5′-GMP (guanosine-5′-mono-phosphate), while the adduct of PtL3Cl with 5′-GMP could not be found in the ES-MS spectra due to the steric effect. The more DNA intercalative effect of PtL3Cl has been correlated with its larger planar coordination plan, while the covalent binding effect of PtL1Cl and PtL2Cl to the nucleotide prevented their intercalation into DNA base pairs. In vitro data demonstrated that PtL3Cl exhibited the highest cytotoxicity than the other two complexes against the Hela cell line. |
| Keywords: pyrazolyl-Pt(Ⅱ) DNA-binding cytotoxicity |
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| 姜 琴,施鹏飞,朱建辉.单功能铂配合物的合成表征、DNA结合和抗肿瘤活性(英文)[J].无机化学学报,2009,25(10):1764-1770. |
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