Synthesis and biological results of the technetium-99m-labeled 4-nitroimidazole for imaging tumor hypoxia

被引:46
作者
Chu, TW
Hu, SW
Wei, B
Wang, Y
Liu, XQ
Wang, XY [1 ]
机构
[1] Peking Univ, Coll Chem & Mol Engn, Dept Appl Chem, Beijing 100871, Peoples R China
[2] Peking Univ, Coll Life Sci, Beijing 100871, Peoples R China
基金
中国国家自然科学基金;
关键词
4-nitroimidazole; hypoxia imaging agent; biodistribution; tumor;
D O I
10.1016/j.bmcl.2003.11.017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
1-(4-Nitroimidazole-1-yl)-propanhydroxyiminoamide (N41PA) was synthesized. The biodistribution of Tc-99m-N41PA in mice bearing S180 tumor demonstrated that the complex showed accumulation in tumor and slow clearance from it. The tumor-to-tissue uptake ratios increase with time. These results suggest that Tc-99m-N41PA would be a marker for imaging tumor hypoxia. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:747 / 749
页数:3
相关论文
共 10 条
  • [1] Cook GJR, 1998, EUR J NUCL MED, V25, P335
  • [2] 99mTc-labeling studies of a modified metronidazole and its biodistribution in tumor bearing animal models
    Das, T
    Banerjee, S
    Samuel, G
    Sarma, HD
    Korde, A
    Venkatesh, M
    Pillai, MRA
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2003, 30 (02) : 127 - 134
  • [3] CHEMISTRY OF AMIDOXIMES AND RELATED COMPOUNDS
    ELOY, F
    LENAERS, R
    [J]. CHEMICAL REVIEWS, 1962, 62 (02) : 155 - &
  • [4] SYNTHESIS, CHARACTERIZATION, AND IN-VITRO EVALUATION OF NITROIMIDAZOLE BATO COMPLEXES - NEW TECHNETIUM COMPOUNDS DESIGNED FOR IMAGING HYPOXIC TISSUE
    LINDER, KE
    CHAN, YW
    CYR, JE
    NOWOTNIK, DP
    ECKELMAN, WC
    NUNN, AD
    [J]. BIOCONJUGATE CHEMISTRY, 1993, 4 (05) : 326 - 333
  • [5] HYDROXAMAMIDE AS A CHELATING MOIETY FOR THE PREPARATION OF TC-99M RADIOPHARMACEUTICALS .2. THE TC-99M COMPLEXES OF HYDROXAMAMIDE DERIVATIVES
    NAKAYAMA, M
    SAIGO, H
    KODA, A
    OZEKI, K
    HARADA, K
    SUGII, A
    TOMIGUCHI, S
    KOJIMA, A
    HARA, M
    NAKASHIMA, R
    OHYAMA, Y
    TAKAHASHI, M
    TAKATA, J
    KARUBE, Y
    [J]. APPLIED RADIATION AND ISOTOPES, 1994, 45 (06) : 735 - 740
  • [6] NITROIMIDAZOLES AND IMAGING HYPOXIA
    NUNN, A
    LINDER, K
    STRAUSS, HW
    [J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE, 1995, 22 (03): : 265 - 280
  • [7] Nitroimidazoles and hypoxia imaging:: Synthesis of three Technetium-99m complexes bearing a nitroimidazole group:: Biological results
    Riché, F
    d'Hardemare, AD
    Sèpe, S
    Riou, L
    Fagret, D
    Vidal, M
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (01) : 71 - 74
  • [8] HYDROXYMETHYLATION AND CYANOETHYLATION OF NITROIMIDAZOLES
    SEHGAL, RK
    AGRAWAL, KC
    [J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1979, 16 (05) : 871 - 876
  • [9] Noninvasive assessment of tumor hypoxia with 99mTc labeled metronidazole
    Yang, DJ
    Ilgan, S
    Higuchi, T
    Zareneyrizi, F
    Oh, CS
    Liu, CW
    Kim, EE
    Podoloff, DA
    [J]. PHARMACEUTICAL RESEARCH, 1999, 16 (05) : 743 - 750
  • [10] ELECTRON-AFFINIC RADIOSENSITIZERS POSSESSING NPSH-REACTIVE SIDE-CHAINS - CYTOTOXICITY AND RADIOSENSITIZING ACTIVITY TOWARDS HYPOXIC EMT6 CELLS IN-VITRO
    ZHOU, L
    NISHIMOTO, SI
    [J]. INTERNATIONAL JOURNAL OF RADIATION BIOLOGY, 1995, 67 (03) : 335 - 346