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

Pharmaceuticals

Hans-Jörg Breyholz¹  Stefan Wagner¹  Klaus Kopka²  Michael Schäfers³ 

[1] Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany;Division of Radiopharmaceutical Chemistry, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, D-69120 Heidelberg, Germany;European Institute for Molecular Imaging (EIMI), University of Münster, Waldeyerstraße 15, D-48149 Münster, Germany;

关键词: pyrimidine-2,4,6-triones;    radioiodination;    matrix metalloproteinase inhibitor;    fluorometric in vitro inhibition assays;   

DOI  :  10.3390/ph10020049

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown