Carbon-11 labelling of an N-sulfonylamino acid derivative: a potential tracer for MMP-2 and MMP-9 imaging

✍ Scribed by Bertrand Kuhnast; Claudia Bodenstein; Hans Jürgen Wester; Wolfang Weber

• Publisher: John Wiley and Sons
• Year: 2003
• Tongue: French
• Weight: 148 KB
• Volume: 46
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.695

✦ Synopsis

Abstract

Matrix metalloproteinases (MMPs) are a family of proteinases that play an important role in cancer. Non invasive imaging of MMPs would allow the evaluation of MMP activity in cancer and the assessment of the response of MMP inhibitor based therapies. In this paper, we investigated the synthesis and labelling by methylation with [^11^C]CH~3~I of an N‐sulfonylamino acid derivative, the (2R)‐3‐methyl‐2‐[[4‐[(4‐methoxybenzoyl)amino]benzenesulfonyl]amino] butanoic acid, a selective and high potent MMP‐2 and MMP‐9 inhibitor, for cancer imaging with positron emission tomography. Labelling of (2R)‐3‐methyl‐2‐[[4‐[(4‐hydroxybenzoyl)amino]benzenesulfonyl] amino] butanoic acid was carried out in a radiochemical yield of 50%–60% within 40 min with a specific activity of 11–26 GBq/µmol (EOS). In vitro inhibitory activity studies, biodistribution and in vivo serum stability in normal mice are also described. Copyright © 2003 John Wiley & Sons, Ltd.