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Molecules 2011, 16(8), 6165-6178; doi:10.3390/molecules16086165

Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents

Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
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Received: 10 June 2011 / Revised: 15 July 2011 / Accepted: 19 July 2011 / Published: 25 July 2011
(This article belongs to the Special Issue Radical Chemistry)
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Abstract

A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of 99mTc-MIPrDP, 99mTc-MIBDP and 99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer 99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that 99mTc-MIPrDP holds great potential for use in bone imaging.
Keywords: zoledronic acid derivative; 99mTc-labelled diphosphonates; in vitro stability; biodistribution; bone imaging agent zoledronic acid derivative; 99mTc-labelled diphosphonates; in vitro stability; biodistribution; bone imaging agent
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Qiu, L.; Cheng, W.; Lin, J.; Luo, S.; Xue, L.; Pan, J. Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents. Molecules 2011, 16, 6165-6178.

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