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Synthesis of a radioiodinated thymidine phosphorylase inhibitor and its preliminary evaluation as a potential SPECT tracer for angiogenic enzyme expression
Author(s) -
Takahashi Masayuki,
Seki Kohichi,
Nishijima Kenichi,
Zhao Songji,
Kuge Yuji,
Tamaki Nagara,
Ohkura Kazue
Publication year - 2008
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1544
Subject(s) - chemistry , thymidine phosphorylase , in vivo , thymidine , enzyme , specific activity , yield (engineering) , radiochemistry , hydrochloride , angiogenesis , pharmacokinetics , in vitro , high performance liquid chromatography , biochemistry , pharmacology , chromatography , cancer research , materials science , microbiology and biotechnology , metallurgy , biology , medicine
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.