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 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 <SC>D</SC>-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 © 2002 John Wiley & Sons, Ltd.