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Bioorg Med Chem. 2008 Feb 15;16(4):1648-57. Epub 2007 Nov 17.

Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer.

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  • 1Department of Chemistry and Biochemistry and Notre Dame Cancer Research Center, University of Notre Dame, Notre Dame, IN 46556, USA.


A siderophore conjugate was designed as a potential PSMA inhibitor and diagnostic agent for prostate cancer. A semi-rigid spacer was incorporated to avoid competitive participation of iron binding by the enzyme inhibitor relative to the siderophore component. Biological test results showed that, even with the extended scaffold, this compound is a potent PSMA inhibitor with an IC50 of 4 nM. This siderophore conjugate may be useful for detection of prostate-derived cancer cells by magnetic resonance imaging (MRI).

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