Design and synthesis of fluorine-18 labeled matrix metalloproteinase inhibitors for cancer imaging

Shozo Furumoto, Ren Iwata, Tatsuo Ido

Research output: Contribution to journalArticlepeer-review

27 Citations (Scopus)

Abstract

Matrix metalloproteinases (MMPs) are key enzymes involved in cancer invasion and metastasis. New 18F-labeled MMP inhibitors (1a-c) has been designed and synthesized for cancer imaging by positron emmision tomography. The precursors were synthesized in four steps starting from D-form of amino acids. Radiosynthesis of 1a-c were carried out by simple one-pot synthesis. The resulting radiofluorinated MMP inhibitors were obtained in overall radiochemical yields of 13-43% (EOB, decay corrected) within 60-70 min (including final preparative HPLC separation).

Original languageEnglish
Pages (from-to)975-986
Number of pages12
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume45
Issue number11
DOIs
Publication statusPublished - 2002 Oct 15

Keywords

  • Fluorine-18
  • Inhibitor
  • Matrix metalloproteinase
  • Pet
  • Tumor imaging

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology

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