共 23 条
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.
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页码:260 / 266
页数:7
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