Synthesis and biological evaluation of novel 99mTc labeled ornidazole xanthate complexes as potential hypoxia imaging agents

被引:11
作者
Li, Zhenxiang [1 ]
Song, Xiaoqing [1 ]
Zhang, Junbo [1 ]
机构
[1] Beijing Normal Univ, Coll Chem, Key Lab Radiopharmaceut, Minist Educ, Beijing 100875, Peoples R China
基金
北京市自然科学基金; 中国国家自然科学基金;
关键词
Ornidazole; Xanthate; Tc-99m; Hypoxia; Tumor imaging; IN-VIVO; DEOXYGLUCOSE DITHIOCARBAMATE; TUMOR; BIODISTRIBUTION; MARKER; VITRO; DERIVATIVES; BEARING;
D O I
10.1007/s10967-015-4125-2
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
In this study, ornidazole xanthate (ONXT) ligand was successfully synthesized and its Tc-99m-nitrido core, Tc-99m-oxo core and [Tc-99m(CO)(3)](+) core complexes were prepared with high yields. The tumor cell experiments and the biodistribution in mice bearing S180 tumor showed that all of the complexes had a certain hypoxic selectivity and tumor uptake. Among them, (TcO)-Tc-99m-ONXT exhibited the highest tumor uptake and tumor/muscle ratio. Planar scintigraphic imaging studies showed the tumor detection was observable, suggesting it would be a potential radiotracer to target tumor hypoxia.
引用
收藏
页码:535 / 542
页数:8
相关论文
共 27 条
  • [1] Ballinger JR, 1996, J NUCL MED, V37, P1023
  • [2] Imaging hypoxia in tumors
    Ballinger, JR
    [J]. SEMINARS IN NUCLEAR MEDICINE, 2001, 31 (04) : 321 - 329
  • [3] Preparation and biodistribution of technetium-99m-labeled 1-(2-nitroimidazole-1-yl)-propanhydroxyimino amide (N21PA) as a tumor hypoxia marker
    Chu, TW
    Li, RJ
    Hu, SW
    Liu, XQ
    Wang, XY
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2004, 31 (02) : 199 - 203
  • [4] Influence of ligand denticity on the properties of novel 99mTc(I)-carbonyl complexes. Application to the development of radiopharmaceuticals for imaging hypoxic tissue
    Fernandez, Soledad
    Giglio, Javier
    Rey, Ana M.
    Cerecetto, Hugo
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2012, 20 (13) : 4040 - 4048
  • [5] Synthesis and evaluation of a new 99mTc(I)-tricarbonyl complex bearing the 5-nitroimidazol-1-yl moiety as potential hypoxia imaging agent
    Giglio, J.
    Dematteis, S.
    Fernandez, S.
    Cerecetto, H.
    Rey, A.
    [J]. JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2014, 57 (06) : 403 - 409
  • [6] Synthesis, in vitro and in vivo characterization of novel 99mTc-'4+1'-labeled 5-nitroimidazole derivatives as potential agents for imaging hypoxia
    Giglio, Javier
    Fernandez, Soledad
    Pietzsch, Hans-Juergen
    Dematteis, Sylvia
    Moreno, Maria
    Pacheco, Jose P.
    Cerecetto, Hugo
    Rey, Ana
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2012, 39 (05) : 679 - 686
  • [7] Synthesis and biological characterisation of novel dithiocarbamate containing 5-nitroimidazole 99mTc-complexes as potential agents for targeting hypoxia
    Giglio, Javier
    Fernandez, Soledad
    Rey, Ana
    Cerecetto, Hugo
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (01) : 394 - 397
  • [8] Syntheses of 2-Nitroimidazole Derivatives Conjugated with 1,4,7-Triazacyclononane-N,N′-Diacetic Acid Labeled with F-18 Using an Aluminum Complex Method for Hypoxia Imaging
    Hoigebazar, Lathika
    Jeong, Jae Min
    Lee, Ji-Youn
    Shetty, Dinesh
    Yang, Bo Yeun
    Lee, Yun-Sang
    Lee, Dong Soo
    Chung, June-Key
    Lee, Myung Chul
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (07) : 3155 - 3162
  • [9] Synthesis and biological evaluation of a novel 99mTc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia
    Joyard, Yoann
    Le Joncour, Vadim
    Castel, Helene
    Diouf, Cherif Bounana
    Bischoff, Laurent
    Papamicael, Cyril
    Levacher, Vincent
    Vera, Pierre
    Bohn, Pierre
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (13) : 3704 - 3708
  • [10] Lewis JS, 1999, J NUCL MED, V40, P177