Synthesis, Radiosynthesis, and Biological Evaluation of New Proteasome Inhibitors in a Tumor Targeting Approach

Proteasome inhibition is a new strategy in cancer therapy. We synthesized three new peptide aldehyde inhibitors linked to the benzamide derivative structure to use their cytotoxic activity against malignant melanoma cells. Of these, <b>10</b> displayed the highest cytotoxicity (0.18 ± 0.16 µM). A radiosynthesis of the iodine aldehyde was performed. Its drug biodistribution showed that some selectivity of the benzamide group toward malignant melanoma tissue was conserved.