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Novel seven-membered ring-fused naphthalimide derivatives with potentials for cancer theranostics    

文献类型:期刊文献

中文题名:Novel seven-membered ring-fused naphthalimide derivatives with potentials for cancer theranostics

作者:Yonghui Yang[1];Xiayu Shi[1];Zhuo Chen[1];Yufang Xu[1];Xuhong Qian[1];Weiping Zhu[1]

机构:[1]State Key Laboratory of Bioreactor Engineering,Shanghai Key Laboratory of Chemical Biology,Shanghai key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China

年份:2023

卷号:34

期号:4

起止页码:236

中文期刊名:Chinese Chemical Letters

外文期刊名:中国化学快报(英文版)

收录:CSTPCD;;Scopus;CSCD:【CSCD2023_2024】;PubMed;

基金:the National Natural Science Foundation of China(Nos. 21878088, 21476077);Key Project of the Shanghai Science and Technology Committee (No. 18DZ1112703) for financial support。

语种:英文

中文关键词:Seven-membered ring;Antitumor activity;High fluorescent quantum yield;Theranostics

摘要:Naphthalimide derivatives have good planarity and large conjugated structure and therefore possess photophysical properties and biological activities. Previously, our group discovered seven-membered heterocyclic derivatives via modifying 4-and 5-positions of naphthalimide skeleton and found the derivatives had good water solubility and showed large stokes shift and strong fluorescence in water. In this article, we designed and synthesized more seven-membered ring-fused naphthalimide derivatives(Y1-Y16)by introducing different substitutions on the imide group. Among them, Y1, Y5, Y9 were found to show similar cytotoxic activities with Amonafide against A549 and HL60 cells, with IC50values at 10^(-6)mol/L.What is more, the asymmetry derivatives(Y1 and Y5) showed high fluorescent quantum yields in the aqueous phase(Ф = 0.47). Considering the great fluorescence quantum yields in water and the potent anti-tumor activities of the representative seven-membered ring-fused naphthalimides, they have potentials to be used as agents for cancer theranostics.

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