Prostate-specific membrane antigen (PSMA) provides an attractive target for the development of targeted chemotherapeutics for prostate cancer. We have designed and synthesized a bioconjugate 1 that comprises the cytotoxic drug doxorubicin and one of our previously described urea-based PSMA inhibitors. While this bioconjugate retained high binding affinity for PSMA, it inhibited only 30 % of C4-2 cell growth at a concentration of 5.0 μM.
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Jayaprakash et al. (2006) studied this question.
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