Synthesis of triazenes by using aryl diazonium silica sulfates under mild conditions

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, 10 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.

Malcolm F. G. Stevens

Papers

Selective Reactions in the Triazene Series; I. Reduction of 1-(4-Acetylphenyl)-triazenes