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

Matrix metalloproteinases (MMPs) are key enzymes involved in cancer invasion and metastasis. New F-18-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). Copyright (C) 2002 John Wiley Sons, Ltd.