Abstract

AbstractThe 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.

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