Preparation and Preliminary Biological Evaluation of Novel 99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents 英文参考文献.docVIP
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Preparation and Preliminary Biological Evaluation of Novel 99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents 英文参考文献
Molecules 2012, 17, 8518-8532; doi:10.3390/moleculeOPEN ACCESS
molecules
ISSN 1420-3049
/journal/molecules
Article
Preparation and Preliminary Biological Evaluation of Novel
99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents
Chunxiong Lu 1,2,*, Quanfu Jiang 1, Cheng Tan 1, Jie Tang 1 and Jiankang Zhang 1
1
Key Laboratory of Nuclear Medicine, Ministry of Health-Jiangsu Key Laboratory of Molecular
Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
2
School of Chemical and Material Engineering, Jiangnan University, Wuxi 214122, China
* Author to whom correspondence should be addressed; E-Mail: luchunxiong@;
Tel.: +86-0510-8551-4482; Fax: +86-0510-8551-3113.
Received: 18 May 2012; in revised form: 27 June 2012 / Accepted: 5 July 2012 /
Published: 16 July 2012
Abstract: Two kinds of novel thymidine derivatives, N-thymidine-yl-N′-methyl-N′-{N′′-
[2-sulfanyl-(ethylamino)acetyl]-2-aminoethylsulfanyl-1-hexanamide}-ethanediamine
(TMHEA)
and
N-thymidine-yl-N′-methyl-N′-{N′′-[2-sulfanyl-(ethylamino)acetyl]-2-
aminoethylsulfanyl-1-hexanamide}-hexanediamine
(TMHHA)
were
prepared
and
successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo
biodistribution of 99mTc-TMHEA and 99mTc-TMHHA were investigated and compared.
The biodistribution studies indicate that the radiotracer 99mTc-TMHEA displays selective
tumor uptake, suggesting it is a potential tumor imaging agent.
Keywords: thymidine derivative; 99mTc-labelled; biodistribution; tumor imaging
1. Introduction
In clinical oncology, 2′-deoxy-2′-[18F]fluoro-D-glucose (18F-FDG), a glucose derivative, has been
widely used in recent years for tumor imaging with positron emission tomography (PET). However,
18F-FDG is a non-specific tracer for tumor imaging since glucose is highly utilized by many other
cells, such as macrophages found in inflammatory lesions [1,2]. To overcome this inconvenience of
18F-FD
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