Synthesis, G-quadruplex binding properties and cytotoxicity of naphthalimide-thiourea conjugates

	Synthesis, G-quadruplex binding properties and cytotoxicity of naphthalimide-thiourea conjugates
	Ou, Zhize 1; Xu, Moheng 1; Gao, Yunyan 1; Hu, Rui 2; Li, Qingqing 1; Cai, Wenjiao 1; Wang, Ziji 1; Qian, Yimeng 1; Yang, Guoqiang 2
刊名	NEW JOURNAL OF CHEMISTRY
	2017-09-07
卷号	41 期号:17 页码:9397-9405
英文摘要	Four novel naphthalimide-thiourea conjugates 3a-d have been prepared and characterized. The interactions of these compounds with duplex and telomeric G-quadruplex DNA have been investigated by UV-Vis spectroscopy, fluorescence spectroscopy, viscosity and cyclic voltammetric measurements. The studies reveal that 3a-d possess high affinity (>1.20 x 10(7) M-1) and reasonable selectivity for telomeric G-quadruplex DNA over duplex DNA. Viscosity and cyclic voltammetric experiments suggest that 3a-d bind to duplex DNA through a classical intercalation mode. Molecular docking studies indicate that 3a-d associate with telomeric G-quadruplexes through groove binding, and hydrogen bonding interactions exist between the thiourea moiety and the phosphates or the bases in the G-quadruplex. The emissive nature of compounds 3a-d makes it possible to study their localization in A549 cells by fluorescence microscopy. The representative compounds 3d and 3b are mainly localized in the nuclei after 4 h of incubation. All four compounds inhibit A549 cells selectively over normal HUVEC cells, with a higher antitumor activity than amonafide.
语种	英语
内容类型	期刊论文
源URL	[http://ir.iccas.ac.cn/handle/121111/41250]
专题	化学研究所_光化学实验室
作者单位	1.Northwestern Polytech Univ, Sch Sci, Dept Appl Chem, Key Lab Space Appl Phys & Chem,Minist Educ, Xian 710072, Peoples R China 2.Chinese Acad Sci, Inst Chem, CAS Key Lab Photochem, Beijing 100190, Peoples R China
推荐引用方式 GB/T 7714	Ou, Zhize,Xu, Moheng,Gao, Yunyan,et al. Synthesis, G-quadruplex binding properties and cytotoxicity of naphthalimide-thiourea conjugates[J]. NEW JOURNAL OF CHEMISTRY,2017,41(17):9397-9405.
APA	Ou, Zhize.,Xu, Moheng.,Gao, Yunyan.,Hu, Rui.,Li, Qingqing.,...&Yang, Guoqiang.(2017).Synthesis, G-quadruplex binding properties and cytotoxicity of naphthalimide-thiourea conjugates.NEW JOURNAL OF CHEMISTRY,41(17),9397-9405.
MLA	Ou, Zhize,et al."Synthesis, G-quadruplex binding properties and cytotoxicity of naphthalimide-thiourea conjugates".NEW JOURNAL OF CHEMISTRY 41.17(2017):9397-9405.