Synthesis of a radioiodinated thymidine phosphorylase inhibitor and its preliminary evaluation as a potential SPECT tracer for angiogenic enzyme expression
| Autor: | Songji Zhao, Masayuki Takahashi, Koh-ichi Seki, Ken-ichi Nishijima, Yuji Kuge, Nagara Tamaki, Kazue Ohkura |
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| Rok vydání: | 2008 |
| Předmět: |
chemistry.chemical_classification
Biodistribution Angiogenesis Hydrochloride Organic Chemistry Biochemistry Chemical synthesis Analytical Chemistry chemistry.chemical_compound Enzyme chemistry In vivo Drug Discovery Radiology Nuclear Medicine and imaging Specific activity Thymidine phosphorylase Spectroscopy |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 51:384-387 |
| ISSN: | 1099-1344 0362-4803 |
| Popis: | The expression of thymidine phosphorylase (TP) is strongly associated with angiogenesis in tumors and activation of antitumor agents. We designed a novel 5-125I-labeled 6-(2-iminoimidazolidinyl)methyluracil hydrochloride ([125I]5I6IMU-HCl) to develop an effective radiotracer for in vivo assessment of TP expression in tumors and prognosis of cancer chemotherapy. Radiotracer synthesis was achieved by radioiodination of the precursor, 6-(2-iminoimidazolidinyl)methyluracil at the C-5 position with NCS/radioiodide. After purification by HPLC, [125I]5I6IMU-HCl was obtained in high radiochemical yield with satisfactory specific activity. The radiotracer showed high inhibitory potency for the target enzyme and good stability in vivo. Copyright © 2008 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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