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新型萘二甲酰亚胺脂肪族氮氧化物作为实体瘤中缺氧细胞的荧光标记物

Novel aliphatic N-oxide of naphthalimides as fluorescent markers for hypoxic cells in solid tumor.

作者信息

Yin Hong, Zhu Weiping, Xu Yufang, Dai Min, Qian Xuhong, Li Yuanli, Liu Jianwen

机构信息

Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China.

出版信息

Eur J Med Chem. 2011 Jul;46(7):3030-7. doi: 10.1016/j.ejmech.2011.04.040. Epub 2011 Apr 21.

DOI:10.1016/j.ejmech.2011.04.040
PMID:21550698
Abstract

A series of novel aliphatic N-oxide of naphthalimides (A1-A5) were designed and prepared. The N-O group was firstly introduced into the amine side chain tailed to planar naphthalimide chromophore as hypoxic bioreductive marker. Fluorescence image analysis showed that the compounds could be used as potential markers for hypoxic cells (V79) in vitro especially for A1 with 17 times hypoxic-oxic fluorescence differential, which was probably due to the bis-bioreduction mechanism.

摘要

设计并制备了一系列新型萘二甲酰亚胺脂肪族氮氧化物(A1 - A5)。首次将N - O基团引入到连接在平面萘二甲酰亚胺发色团上的胺侧链中,作为低氧生物还原标记物。荧光图像分析表明,这些化合物可作为体外低氧细胞(V79)的潜在标记物,尤其是A1,其低氧 - 常氧荧光差异达17倍,这可能归因于双生物还原机制。

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