Syntheses of radioiodinated pyrimidine-2,4,6-triones as potential agents for non-invasive imaging of matrix metalloproteinases

Breyholz H., Kopka K., Schäfers M., Wagner S.

Research article (journal) | Peer reviewed

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.

Details about the publication

JournalPharmaceuticals
Volume10
Issue2
StatusPublished
Release year2017
Language in which the publication is writtenEnglish
DOI10.3390/ph10020049
Link to the full texthttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85020755797&origin=inward
KeywordsFluorometric in vitro inhibition assays; Matrix metalloproteinase inhibitor; Pyrimidine-2,4,6-triones; Radioiodination

Authors from the University of Münster

Breyholz, Hans-Jörg
Clinic for Nuclear Medicine