文献类型：期刊文献

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

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

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai key Lab New Drug Design, State Key Lab Bioreactor Engn,Shanghai Key Lab Che, Shanghai 200237, Peoples R China

年份：2023

卷号：34

期号：4

外文期刊名：CHINESE CHEMICAL LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000925416700001)】；

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

语种：英文

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

摘要：Naphthalimide derivatives have good planarity and large conjugated structure and therefore possess pho-tophysical properties and biological activities. Previously, our group discovered seven-membered hetero-cyclic 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 arti-cle, 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 IC50 values at 10 -6 mol/L. What is more, the asymmetry derivatives ( Y1 and Y5 ) showed high fluorescent quantum yields in the aqueous phase ( CYRILLIC CAPITAL LETTER EF = 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 poten-tials to be used as agents for cancer theranostics.(c) 2023 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.