Abstract:Prostate-specific membrane antigen (PSMA) overexpressed on prostate cancer (PCa) cells is a satisfactory theranostic target in PCa. To seek novel non-glutamate-ureabased PSMA inhibitors by the strategy of bioisosterism, 10 ligands were designed, synthesized, and characterized. Among them, ligands 17, 18, and 21−24 bearing the squaramic acid moiety proved to be potent PSMA inhibitors, with K i values ranging from 0.40 to 2.49 nM, which are comparable or higher in inhibitory potency compared to previously report… Show more
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