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口占吨酮衍生物的合成及与G-四链体作用的研究
Synthesis of Xanthone Derivatives and Its Interaction with G-quadruplex

作  者: ; ; ; ; ; ;

机构地区: 广西师范大学化学化工学院省部共建药用资源化学与药物分子工程教育部重点实验室

出  处: 《广西师范大学学报(自然科学版)》 2009年第4期65-69,共5页

摘  要: 以邻羟基苯甲酸和间苯三酚为原料,通过一步法合成了1,3-二羟基口占吨酮,再经醚化、取代、季铵化反应得到化合物d,用IR、NMR、MS、元素分析等进行结构测定和表征,利用圆二色(CD)光谱和变温紫外-可见(UV-Vis)光谱研究了化合物d与G-四链体DNA的相互作用。CD光谱表明化合物d能诱导端粒DNA片段d[G3(T2AG3)3]形成反平行型的G-四链体结构;变温UV-Vis光谱显示化合物d使相应G-四链体DNA的Tm值增加约6°C,表明化合物d同时起到稳定G-四链体的作用。 1,3-Dihydroxyxanthone was synthesized by condensation of salicylic acid and phloroglucinol in one step,and then etherification,substitution and quaternization reaction took place successively to offer xanthone derivatives ft. The compounds were determined and characterized by IR, NMR, MS and elemental analysis. Circular dichroism (CD) and UV-Vis spectrum were employed for preliminary investigating the interaction between compound d and G-quadruplex. CD spectrum suggested that compound d could induce d EG3(T2AG3)3JDNA to form anti-parallel G-quadruplex in vitro. And the melting profile by UV-Vis spectrum indicated that compound fl also could enhance the Tm of corresponding quadruplex DNA up to about 6℃,which suggested that compound d were capable of stabilizing G-quadruplex DNA.

关 键 词: 呫吨酮 季铵盐 四链体

领  域: [化学工程] [化学工程]

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