Dinitro Derivative of Naphthalimide as a Fluorescent Probe for Tumor Hypoxia Imaging

Author(s):  
Rashmi Kumari ◽  
Vasumathy R. ◽  
Dhanya Sunil ◽  
Anil Kumar N. V. ◽  
Raghumani Singh Ningthoujam ◽  
...  
2015 ◽  
Vol 51 (79) ◽  
pp. 14739-14741 ◽  
Author(s):  
Qi Cai ◽  
Tao Yu ◽  
Weiping Zhu ◽  
Yufang Xu ◽  
Xuhong Qian

A turn-on fluorescent probe was designed and synthesized for tumor hypoxia imaging, which could show excellent reducing ability under chemical or bio-reductase conditions and good performance in hypoxia imaging for HeLa cells at different oxygen concentrations.


Nanoscale ◽  
2020 ◽  
Vol 12 (14) ◽  
pp. 7509-7513 ◽  
Author(s):  
Tianhao Xue ◽  
Kuanchun Shao ◽  
Jingyuan Xiang ◽  
Xinyi Pan ◽  
Zixuan Zhu ◽  
...  

A novel hypoxia-responsive fluorescent probe of a hydrophilic azobenzene containing copolymer combined with a carbamate linkage and anionic water-soluble tetraphenylethene by using the in situ self-assembly concept for tumor hypoxia imaging is reported.


2011 ◽  
Vol 6 (1) ◽  
pp. 165 ◽  
Author(s):  
Florian C Maier ◽  
Manfred Kneilling ◽  
Gerald Reischl ◽  
Funda Cay ◽  
Daniel Bukala ◽  
...  

2019 ◽  
Vol 12 (1) ◽  
pp. 31
Author(s):  
Florian Maier ◽  
Anna Schweifer ◽  
Vijaya Damaraju ◽  
Carol Cass ◽  
Gregory Bowden ◽  
...  

The benefits of PET imaging of tumor hypoxia in patient management has been demonstrated in many examples and with various tracers over the last years. Although, the optimal hypoxia imaging agent has yet to be found, 2-nitroimidazole (azomycin) sugar derivatives—mimicking nucleosides—have proven their potential with [18F]FAZA ([18F]fluoro-azomycin-α-arabinoside) as a prominent representative in clinical use. Still, for all of these tracers, cellular uptake by passive diffusion is postulated with the disadvantage of slow kinetics and low tumor-to-background ratios. We recently evaluated [18F]fluoro-azomycin-β-deoxyriboside (β-[18F]FAZDR), with a structure more similar to nucleosides than [18F]FAZA and possible interaction with nucleoside transporters. For a deeper insight, we comparatively studied the interaction of FAZA, β-FAZA, α-FAZDR and β-FAZDR with nucleoside transporters (SLC29A1/2 and SLC28A1/2/3) in vitro, showing variable interactions of the compounds. The highest interactions being for β-FAZDR (IC50 124 ± 33 µM for SLC28A3), but also for FAZA with the non-nucleosidic α-configuration, the interactions were remarkable (290 ± 44 µM {SLC28A1}; 640 ± 10 µM {SLC28A2}). An improved synthesis was developed for β-FAZA. For a PET study in tumor-bearing mice, α-[18F]FAZDR was synthesized (radiochemical yield: 15.9 ± 9.0% (n = 3), max. 10.3 GBq, molar activity > 50 GBq/µmol) and compared to β-[18F]FAZDR and [18F]FMISO, the hypoxia imaging gold standard. We observed highest tumor-to-muscle ratios (TMR) for β-[18F]FAZDR already at 1 h p.i. (2.52 ± 0.94, n = 4) in comparison to [18F]FMISO (1.37 ± 0.11, n = 5) and α-[18F]FAZDR (1.93 ± 0.39, n = 4), with possible mediation by the involvement of nucleoside transporters. After 3 h p.i., TMR were not significantly different for all 3 tracers (2.5–3.0). Highest clearance from tumor tissue was observed for β-[18F]FAZDR (56.6 ± 6.8%, 2 h p.i.), followed by α-[18F]FAZDR (34.2 ± 7.5%) and [18F]FMISO (11.8 ± 6.5%). In conclusion, both isomers of [18F]FAZDR showed their potential as PET hypoxia tracers. Differences in uptake behavior may be attributed to a potential variable involvement of transport mechanisms.


2020 ◽  
Vol 63 (12) ◽  
pp. 1786-1797 ◽  
Author(s):  
Fengfeng Xue ◽  
Jufeng Chen ◽  
Hangrong Chen

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1143-1148 ◽  
Author(s):  
Zhenxiang Li ◽  
Junbo Zhang ◽  
Zhonghui Jin ◽  
Weifang Zhang ◽  
Yanyan Zhang

99mTcO-N4IPDTC was prepared from a kit without the need for purification and would be a promising hypoxia imaging agent.


2007 ◽  
Vol 55 (7) ◽  
pp. 1142-1144 ◽  
Author(s):  
Hiroyasu Yasuda ◽  
Tomohiro Kaneta ◽  
Yoshihiro Takai ◽  
Katsutoshi Nakayama ◽  
Ren Iwata ◽  
...  

2005 ◽  
Vol 32 (6Part14) ◽  
pp. 2059-2059
Author(s):  
C Ling

2019 ◽  
Vol 321 (3) ◽  
pp. 943-954 ◽  
Author(s):  
Fan Wang ◽  
Xianteng Yang ◽  
Hua Zhu ◽  
Zhi Yang ◽  
Taiwei Chu

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