Approaches to the Synthesis of Double Conjugates of PSMA Ligands with Monomethyl Auristatin E

Abstract: Two different design of conjugates of prostate specific membrane antigen (PSMA) ligands with monomethyl auristatin E were proposed. PSMA ligands were obtained using peptide synthesis approaches. The possibility of obtaining bimodal conjugates of these ligands with two equivalents of monomethyl auristatin E by the azide-alkyne cycloaddition reaction was shown. The possibility of obtaining compounds containing only one equivalent of monomethyl auristatin E in the structure by these methods was analyzed. © Pleiades Publishing, Ltd. 2025.