1225013-27-3Relevant academic research and scientific papers
Synthesis, radiofluorination, and hypoxia-selective studies of FRAZ: A configurational and positional analogue of the clinical hypoxia marker, [18F]-FAZA
Kumar, Piyush,Naimi, Ebrahim,McEwan, Alexander J.,Wiebe, Leonard I.
experimental part, p. 2255 - 2264 (2010/06/17)
The current work evaluates 1-α-d-(2-deoxy-2-fluororibofuranosyl)-2-nitroimidazole (FRAZ), a novel azomycin nucleoside that is a potential radiosensitizer of tumor hypoxia. FRAZ is a ribose analogue of 1-α-d-(2-deoxy-2-fluoroarabinofuranosyl)-2-nitroimidazole ([18F]-FAZA), a clinically used hypoxia marker. Preliminary assessment of the cytotoxicity and hypoxia-specific in vitro binding in HCT-110 colorectal cancer cells indicate that the radiosensitization properties of FRAZ are similar to that of FAZA, with a sensitizer enhancement ratio (SER) of ～1.8. An automated radiosynthesis of [18F]-FRAZ using a commercial automated synthesis unit (ASU) was established (synthesis time ～32 min; radiochemical yield (decay uncorrecetd) ～22%) to facilitate its application in PET-based diagnosis of hypoxic tumors.
NOVEL SUBSTITUTED 2-NITROIMIDAZOLES USEFUL FOR HYPOXIC CELL THERAPY AND IMAGING
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Page/Page column 47, (2010/11/24)
The present invention provides for substituted 2-nitroimidazoles suitable for the therapeutic treatment of hypoxic tissues, particularly for application in radiotherapy, chemosensitization and radiosensitization The present invention further provides subs
