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Pharmaceuticals 2017, 10(2), 49; doi:10.3390/ph10020049

Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases

1
Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany
2
Division of Radiopharmaceutical Chemistry, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, D-69120 Heidelberg, Germany
3
European Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstraße 15, D-48149 Münster, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 8 May 2017 / Revised: 24 May 2017 / Accepted: 28 May 2017 / Published: 30 May 2017
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Abstract

Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for clinical diagnostics using non-invasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. This work includes the organic chemical syntheses and in vitro evaluation of five iodinated barbiturate based MMPIs and the selection of derivative 9 for radiosyntheses of isotopologues [123I]9 potentially useful for MMP SPECT imaging and [124I]9 for MMP PET imaging. View Full-Text
Keywords: pyrimidine-2,4,6-triones; radioiodination; matrix metalloproteinase inhibitor; fluorometric in vitro inhibition assays pyrimidine-2,4,6-triones; radioiodination; matrix metalloproteinase inhibitor; fluorometric in vitro inhibition assays
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Breyholz, H.-J.; Kopka, K.; Schäfers, M.; Wagner, S. Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases. Pharmaceuticals 2017, 10, 49.

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