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Design and synthesis of fluorine‐18 labeled matrix metalloproteinase inhibitors for cancer imaging
Author(s) -
Furumoto Shozo,
Iwata Ren,
Ido Tatsuo
Publication year - 2002
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.616
Subject(s) - chemistry , radiosynthesis , matrix metalloproteinase , positron emission tomography , matrix (chemical analysis) , combinatorial chemistry , matrix metalloproteinase inhibitor , enzyme , metastasis , cancer , radiochemistry , biochemistry , chromatography , nuclear medicine , medicine
Matrix metalloproteinases (MMPs) are key enzymes involved in cancer invasion and metastasis. New 18 F‐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 © 2002 John Wiley & Sons, Ltd.