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Title
Japanese: 
English:Development of a Hypoxia-Selective Near-Infrared Fluorescent Probe for Non-invasive Tumor Imaging 
Author
Japanese: Youssif Bahaa Gamal Mohamed, Okuda Kensuke, Kadonosono Tetsuya, Salem Ola Ibrahim Abdel Razek, Hayallah Alaa Arafat Mohamed, Hussein Mostafa Ahmed, 近藤科江, Nagasawa Hideko.  
English: Youssif Bahaa Gamal Mohamed, Okuda Kensuke, Kadonosono Tetsuya, Salem Ola Ibrahim Abdel Razek, Hayallah Alaa Arafat Mohamed, Hussein Mostafa Ahmed, Kizaka-Kondoh Shinae, Nagasawa Hideko.  
Language English 
Journal/Book name
Japanese: 
English:Chemical and Pharmaceutical Bulletin 
Volume, Number, Page Vol. 60    No. 3    pp. 402-407
Published date Feb. 2016 
Publisher
Japanese: 
English:公益社団法人日本薬学会 
Conference name
Japanese: 
English: 
Conference site
Japanese: 
English: 
DOI https://doi.org/10.1248/cpb.60.402
Abstract A near-infrared fluorochrome, GPU-311, was designed, synthesized and evaluated for its application in non-invasive imaging of tumor hypoxia. Efficient synthesis was achieved by nucleophilic substitution and click chemistry ring using the bifunctional tetraethylene glycol linker 2 containing thiol and azide groups for the conjugation of the propargylated nitroimidazole 1 and the heptamethine cyanine dye 3 bearing a 2-chloro-1-cyclohexenyl ring. GPU-311 exhibited long excitation and emission wavelength (Ex/Em=785/802 nm) and a decent quantum yield (0.05). The water solubility and hydrophilicity of GPU-311 increased. After in vitro treatment of SUIT-2/HRE-Luc pancreatic cancer cells with GPU-311, a higher level of fluorescence was observed selectively in hypoxia than in normoxia. However, in vivo fluorescence imaging of a mouse xenograft model after GPU-311 administration revealed inadequate accumulation of GPU-311 in tumors due to its rapid elimination through the liver.

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