Specifically targeting human telomeric dimeric G-quadruplexes by polyehter-tethered di-berberine derivatives
作者单位：Guangdong Provincial Key Laboratory of New Drug ScreeningSchool of Pharmaceutical SciencesSouthern Medical University
会议名称：《中国化学会第四届卟啉与酞菁学术研讨会》
会议日期：2017年
学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学]
关 键 词：Di-berberine dimeric quadruplex DNA telomere binding selectivity
摘 要：The design and synthesis of binders specifically multiple G-quadruplex units in the 3’-terminal overhang of human telomeric DNA has attracted considerable attention,which will promote to develop some selective anticancer agents with fewer side *** three polyether-tethered di-berberine compounds（1-3） have been prepared and studied on their binding affinity,selectivity and thermal stabilization towards dimeric quadruplex DNA by UV-Vis titrations,electrophoresis,fluorescence spectroscopy,CD spectroscopy and *** 1 with the shortest polyether linker has been found to have higher binding affinity,selectivity and thermal stabilization towards mixed-type dimeric quadruplexes over antiparallel dimeric and monomeric quadruplexes than compounds 2-3 with the longer polyether *** intriguingly,four molecules of compound 1 might externally stack on the end G-quartets of the two mixed-type G-quadruplex units on one dimeric *** addition,these diberberine derivatives displayed good inhibitory activities toward four tumor cell lines.