Preparation and Preliminary Biological Evaluation of Novel 99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents 英文参考文献.docVIP

Preparation and Preliminary Biological Evaluation of Novel 99mTc-Labelled Thymidine Analogs as Tumor Imaging Agents 英文参考文献.doc

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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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