通过两步简单的合成反应,制备了锌的配体化合物(ZSC).并将其与不同构型的G-四联体作用,发现其可以很好的选择性荧光打开检测G-四联体.通过荧光,圆二色谱(CD)等实验的深入研究,表明这个化合物兼具诱导、稳定和荧光打开检测G-四联体的优点.这是第一次报道既可以诱导稳定G-四联体,又可以进行荧光打开检测定量分析G-四联体的锌的salen配体复合物.此外,这个化学试剂还可以将Z型G-四联体转变成平行的G-四联体.这是一个针对G-四联体的选择性的、敏感的和拓扑特异性的探针.这个探针与不同G-四联体的序列之间的相互作用的研究,展示了它可能作为一种抗癌药物的潜力,并且,有望将其用于基于G-四联体的检测方法检测其他生物物质的领域.
G-quadruplexes play vital roles in telomere maintenance and other biological systems. An effective G-quadruplexes stabilizer can be a promising medicine for cancer therapy. Here, a Zinc(II) with salen derivatives as ligands (ZSC) has been prepared through two simple steps syntheses. 2,4-Dihydroxybenzaldehyde (1 equiv.), 1-(2-chloroethyl)pyrrolidine hydrochloride (1 equiv.) and potassium carbonate (2 equiv.) were dissolved in 150 mL acetone. After reflux for 20 b in Ar atmosphere and purification, the product 2-hydroxy-4-(2-(pyrrolidin-l-yl)ethoxy)benzaldehyde was obtained to yield 3.24 g (68.8%) as a pale solid. For the other step, 2-hydroxy-4-(2-(pyrrolidin-1-yl)ethoxy)benzaldehyde (2 equiv.) and diaminomaleonitrile (1 equiv.) were dissolved into l0 mL methanol. After 20 min stirring at 60℃ in dark atmosphere, the Zinc acetate dehydrate (l equiv.) was added in the solution for further 2 h reaction time. The final product Zinc(II)-salen Complex (ZSC) was purified to yield 245 mg (67.7%) as a red powder. The fluorescence, CD spectra are re- ported, giving insight into the intrinsic properties of the compound. The Zinc(II)-salen Complex could simply discriminate G-quadruplex from other DNA conformations such as hairpin, double-stranded DNA and single-stranded DNA by using flu- orescence spectra. To the best of our knowledge, ZSC is the first Zinc(Ⅱ)-salen Complex bearing features of inducing, stabi- lizing, fluorescence-based switch-on detecting G-quadruplex. In addition, ZSC can also change the Z G-quadruplex to paral- lel G-quadruplex. Such a sensitive and topology-specific probe is able to light up G-quadruplexes and gain an excellently quantitative detection of DNA bearing G-quadruplexes sequences. The detailed study of the interactions of ZSC with different topology DNAs has allowed us to build the most vital features that Zinc(Ⅱ)-salen Complex can be a potential anticancer drug and in application to other bioanalytes. In the