2-Nitroimidazole based fluorescent probes for nitroreductase; monitoring reductive stress in cellulo

被引:58
作者
Ao, X. [1 ]
Bright, S. A. [2 ]
Taylor, N. C. [2 ]
Elmes, R. B. P. [1 ]
机构
[1] Natl Univ Ireland, Maynooth Univ, Dept Chem, Maynooth, Co Kildare, Ireland
[2] Trinity Coll Dublin, TBSI, Dublin 2, Ireland
关键词
OFF-ON PROBE; TUMOR HYPOXIA; SELECTIVE DETECTION; CANCER-THERAPY; IMAGING AGENTS; ANTICANCER; DISEASE; TH-302;
D O I
10.1039/c7ob01406f
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Two 2-nitroimidazole-1,8-naphthalimide conjugates, 1 and 2, have been synthesised as fluorescence probes for the detection of reductive stress in HeLa cells. The 4-substituted derivative 1 was shown to act as a highly sensitive and selective substrate for nitroreductase where it exhibited a clear blue to green ratiometric fluorescence response visible to the naked eye. Moreover, biological studies demonstrated 1 could be activated in cellulo where the impact of reductive stress was easily monitored using confocal microscopy and flow cytommetry.
引用
收藏
页码:6104 / 6108
页数:5
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