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Synthesis and Biological Evaluation of Novel 99mTc(CO)3-Labeled Thymidine Analogs as Potential Probes for Tumor Proliferation Imaging

Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
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Academic Editors: Jean Jacques Vanden Eynde and Annie Mayence
Molecules 2016, 21(4), 510; https://doi.org/10.3390/molecules21040510
Received: 31 December 2015 / Revised: 7 April 2016 / Accepted: 12 April 2016 / Published: 19 April 2016
(This article belongs to the Section Medicinal Chemistry)
Achieving a 99mTc labeled thymidine radiotracer for single photon emission tomography (SPECT) is considered to be of interest. In this study, four novel thymidine analogs, 6a, 6b, 6c and 6d, were successfully synthesized via “click reaction” route and then radiolabeled using a [99mTc(CO)3]+ core to prepare the corresponding 99mTc(CO)3 complexes in high yields. These complexes were hydrophilic and had good in vitro stability. Biodistribution of these complexes in mice bearing S180 tumors showed that all of them exhibited accumulation in the tumors, suggesting that they would be potential tumor imaging agents. View Full-Text
Keywords: thymidine analogs; click chemistry; [99mTc(CO)3]+ core; tumor proliferation imaging; macrocyclic triamine thymidine analogs; click chemistry; [99mTc(CO)3]+ core; tumor proliferation imaging; macrocyclic triamine
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Duan, X.; Liu, T.; Zhang, Y.; Zhang, J. Synthesis and Biological Evaluation of Novel 99mTc(CO)3-Labeled Thymidine Analogs as Potential Probes for Tumor Proliferation Imaging. Molecules 2016, 21, 510.

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