Bioorganic & medicinal chemistry

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

P Ding, P Helquist, MJ Miller

文献索引：Ding, Pingyu; Helquist, Paul; Miller, Marvin J. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 4 p. 1648 - 1657

全文：HTML全文

被引用次数: 12

摘要

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 4nM. This siderophore conjugate may be useful for detection of ...