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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

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.

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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 [J].

Das, T ;

Banerjee, S ;

Samuel, G ;

Sarma, HD ;

Korde, A ;

Venkatesh, M ;

Pillai, MRA .

NUCLEAR MEDICINE AND BIOLOGY, 2003, 30 (02) :127-134

[3] CHEMISTRY OF AMIDOXIMES AND RELATED COMPOUNDS [J].

ELOY, F ;

LENAERS, R .

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 [J].

LINDER, KE ;

CHAN, YW ;

CYR, JE ;

NOWOTNIK, DP ;

ECKELMAN, WC ;

NUNN, AD .

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 [J].

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 .

APPLIED RADIATION AND ISOTOPES, 1994, 45 (06) :735-740

[6] NITROIMIDAZOLES AND IMAGING HYPOXIA [J].

NUNN, A ;

LINDER, K ;

STRAUSS, HW .

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 [J].

Riché, F ;

d'Hardemare, AD ;

Sèpe, S ;

Riou, L ;

Fagret, D ;

Vidal, M .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (01) :71-74

[8] HYDROXYMETHYLATION AND CYANOETHYLATION OF NITROIMIDAZOLES [J].

SEHGAL, RK ;

AGRAWAL, KC .

JOURNAL OF HETEROCYCLIC CHEMISTRY, 1979, 16 (05) :871-876

[9] Noninvasive assessment of tumor hypoxia with 99mTc labeled metronidazole [J].

Yang, DJ ;

Ilgan, S ;

Higuchi, T ;

Zareneyrizi, F ;

Oh, CS ;

Liu, CW ;

Kim, EE ;

Podoloff, DA .

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 [J].

ZHOU, L ;

NISHIMOTO, SI .

INTERNATIONAL JOURNAL OF RADIATION BIOLOGY, 1995, 67 (03) :335-346