Synthesis of a [18F]fluoroethyltriazolylthymidine radiotracer from [18F]2-fluoroethyl azide and 5-ethynyl-2′-deoxyuridine

被引:14
作者
Ackermann, U. [1 ,2 ]
O'Keefe, G. [1 ]
Lee, S. -T. [1 ,2 ,3 ]
Rigopoulos, A. [3 ]
Cartwright, G. [3 ]
Sachinidis, J. I. [1 ]
Scott, A. M. [1 ,2 ,3 ]
Tochon-Danguy, H. J. [1 ,2 ]
机构
[1] Austin Hlth, Ctr PET, Melbourne, Vic, Australia
[2] Univ Melbourne, Sch Med Dent & Hlth Sci, Melbourne, Vic, Australia
[3] Ludwig Inst Canc Res, Melbourne Ctr Clin Sci, Heidelberg, Vic, Australia
基金
英国医学研究理事会;
关键词
click chemistry; tumor cell proliferation; thymidine analogue; A431; tumors; POSITRON-EMISSION-TOMOGRAPHY; PROLIFERATION IN-VIVO; CYCLOADDITION; CANCER; CELLS; CLICK; GENE;
D O I
10.1002/jlcr.1863
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
An improved synthesis for a fluoroethyltriazolylthymidine analog has been developed by employing the copper(I)-catalyzed click chemistry reaction between 5-ethynyl-2'-deoxyuridine (EDU) and [F-19/18]2-fluoroethyl azide. When compared with the previously reported protocol the radiochemical yield has been increased from 3 to 32.5 +/- 2.5%. The synthesis time was 130 min and the specific activity ranged from 70.3 to 129.5 GBq/mu mol. The tracer was found to be stable in human plasma and was subsequently evaluated in an A431 tumor model in BALB/c nude mice. Dynamic image acquisition using the Mosaic small animal PET scanner showed that the tumor to muscle ratio reached a maximum value of 2.1 from 22 min postinjection. These results indicate, that the fluoroethyltriazolylthymidine synthesized can be a promising radiotracer for tumor cell proliferation and thus become an important tool for treatment evaluation in oncology.
引用
收藏
页码:260 / 266
页数:7
相关论文
共 23 条
  • [21] Synthesis and properties of 18F-labeled potential myocardial blood flow tracers
    Studenov, AR
    Berridge, MS
    [J]. NUCLEAR MEDICINE AND BIOLOGY, 2001, 28 (06) : 683 - 693
  • [22] Biochemical characterization of mutant EGF receptors expressed in the hemopoietic cell line BaF/3
    Walker, F
    Hibbs, ML
    Zhang, HH
    Gonez, LJ
    Burgess, AW
    [J]. GROWTH FACTORS, 1998, 16 (01) : 53 - 67
  • [23] SYNTHESIS OF 3'-FLUORO-3'-DEOXYTHYMIDINE AND STUDIES OF ITS F-18 RADIOLABELING, AS A TRACER FOR THE NONINVASIVE MONITORING OF THE BIODISTRIBUTION OF DRUGS AGAINST AIDS
    WILSON, IK
    CHATTERJEE, S
    WOLF, W
    [J]. JOURNAL OF FLUORINE CHEMISTRY, 1991, 55 (03) : 283 - 289