Synthesis and bioevaluation of novel radioiodinated PEG-modified 2-nitroimidazole derivatives for tumor hypoxia imaging

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

scholarly journals Significant impact of different oxygen breathing conditions on noninvasive in vivo tumor-hypoxia imaging using [18F]-fluoro-azomycinarabino-furanoside ([18F]FAZA)

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

scholarly journals 2-Nitroimidazole-Furanoside Derivatives for Hypoxia Imaging—Investigation of Nucleoside Transporter Interaction, 18F-Labeling and Preclinical PET Imaging

2019 ◽  
Vol 12 (1) ◽  
pp. 31
Author(s):  
Florian Maier ◽  
Anna Schweifer ◽  
Vijaya Damaraju ◽  
Carol Cass ◽  
Gregory Bowden ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Tumor Hypoxia ◽  
Radiochemical Yield ◽  
Nucleoside Transporters ◽  
Nucleoside Transporter ◽  
Hypoxia Imaging ◽  
Molar Activity ◽  
Slow Kinetics ◽  
Sugar Derivatives

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.

Design strategy of optical probes for tumor hypoxia imaging

2020 ◽  
Vol 63 (12) ◽  
pp. 1786-1797 ◽  
Author(s):  
Fengfeng Xue ◽  
Jufeng Chen ◽  
Hangrong Chen
Keyword(s):  
Tumor Hypoxia ◽  
Design Strategy ◽  
Hypoxia Imaging ◽  
Optical Probes

Synthesis and biodistribution of novel 99mTc labeled 4-nitroimidazole dithiocarbamate complexes as potential agents to target tumor hypoxia

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

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

TUMOR HYPOXIA IMAGING WITH [F-18] FLUORONITROIMIDAZOLE IN NON-SMALL-CELL LUNG CANCER

2007 ◽  
Vol 55 (7) ◽  
pp. 1142-1144 ◽  
Author(s):  
Hiroyasu Yasuda ◽  
Tomohiro Kaneta ◽  
Yoshihiro Takai ◽  
Katsutoshi Nakayama ◽  
Ren Iwata ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Tumor Hypoxia ◽  
Small Cell ◽  
Small Cell Lung ◽  
Hypoxia Imaging

MO-D-J-6C-04: Tumor Hypoxia Imaging

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

A turn-on fluorescent probe for tumor hypoxia imaging in living cells

2015 ◽  
Vol 51 (79) ◽  
pp. 14739-14741 ◽  
Author(s):  
Qi Cai ◽  
Tao Yu ◽  
Weiping Zhu ◽  
Yufang Xu ◽  
Xuhong Qian
Keyword(s):  
Fluorescent Probe ◽  
Hela Cells ◽  
Tumor Hypoxia ◽  
Living Cells ◽  
Hypoxia Imaging ◽  
Turn On ◽  
Reducing Ability ◽  
Oxygen Concentrations

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.

Design of a bioreductively-activated fluorescent pH probe for tumor hypoxia imaging

2009 ◽  
Vol 17 (19) ◽  
pp. 6952-6958 ◽  
Author(s):  
Eiji Nakata ◽  
Yoshihiro Yukimachi ◽  
Hirokazu Kariyazono ◽  
Seongwang Im ◽  
Chiaki Abe ◽  
...  
Keyword(s):  
Tumor Hypoxia ◽  
Hypoxia Imaging ◽  
Ph Probe

Synthesis and biodistribution of 99m Tc-PyDA as a potential marker for tumor hypoxia imaging

2014 ◽  
Vol 56 (1) ◽  
pp. 76-80 ◽  
Author(s):  
T. M. Sakr ◽  
B. M. Essa ◽  
F. A. El-Essawy ◽  
A. A. El-Mohty
Keyword(s):  
Tumor Hypoxia ◽  
Hypoxia Imaging ◽  
Potential Marker
Sign in / Sign up

Export Citation Format

Share Document