论文部分内容阅读
合成了三种2,6-双(N-乙基苯并咪唑)吡啶炔基铂(Ⅱ)配合物(2-4),其中配合物2的炔基配体为抗癌药物埃罗替尼.利用紫外-可见(UV-Vis)吸收光谱,圆二色(CD)光谱,荧光共振能量转移(FRET)等方法研究了铂(Ⅱ)配合物与人体端粒(Hetelo)和c-myc原癌基因(c-myc)G-四链体的相互作用.实验结果表明,所合成的铂配合物与G-四链体具有较强的相互作用(K_a>10~6L·mol~(-1)),在无碱金属离子存在条件下能诱导G-四链体的形成.含苯乙炔基团的配合物2、3能使c-myc G-四链体的熔解温度上升24℃以上,而含丙炔基团的铂配合物4仅使c-myc G-四链体的熔解温度升高9.0℃,表明炔基结构对铂(Ⅱ)配合物与G-四连体的作用有较大影响.配合物2对人肺癌细胞A549的细胞毒性明显高于埃罗替尼及其他两种配合物3、4.
Three kinds of 2,6-bis (N-ethylbenzimidazole) pyridyl alkynylplatinum (Ⅱ) complexes (2-4) were synthesized, in which the alkynyl ligand of the complex 2 was the antitumor drug erlotinib The effects of platinum (Ⅱ) complex with human Hetelo and c-myc were studied by UV-Vis absorption spectroscopy, circular dichroism (CD) spectroscopy and fluorescence resonance energy transfer (FRET) (C-myc) G-quadruplex.The experimental results show that the synthesized platinum complex has a strong interaction with G-quadruplex (K_a> 10 ~ 6L · mol ~ (-1) )) Could induce the formation of G-quadruplexes in the presence of alkali-free metal ions.The complexes 2 and 3 with phenylacetylene groups increased the melting temperature of c-myc G-quadruplex by more than 24 ℃, Whereas the propyne-containing platinum complex 4 only increased the melting temperature of the c-myc G-quadruplex by 9.0 ° C, indicating that the effect of the alkynyl structure on the platinum (II) complex and the G-tetrane is more significant The cytotoxicity of complex 2 to human lung cancer cell A549 was significantly higher than that of erlotinib and other two complexes3,4.