Synthesis of a radioiodinated thymidine phosphorylase inhibitor and its preliminary evaluation as a potential SPECT tracer for angiogenic enzyme expression
✍ Scribed by Masayuki Takahashi; Koh-ichi Seki; Ken-ichi Nishijima; Songji Zhao; Yuji Kuge; Nagara Tamaki; Kazue Ohkura
- Publisher
- John Wiley and Sons
- Year
- 2008
- Tongue
- French
- Weight
- 116 KB
- Volume
- 51
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
The expression of thymidine phosphorylase (TP) is strongly associated with angiogenesis in tumors and activation of antitumor agents. We designed a novel 5‐^125^I‐labeled 6‐(2‐iminoimidazolidinyl)methyluracil hydrochloride ([^125^I]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, [^125^I]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.