Bioorthogonal Gold-Catalyzed Hydrothiolation Leading to Amide Bond Cleavage of Ethynylated Biarylbutanamide Precursors

applications, particularly with the development of prodrug strategies. This work introduces the ethynylated biarylbutanamide (EBB) group, which was designed to undergo gold-catalyzed hydrothiolation, cyclization, and hydrolysis to release amines under mild physiological conditions. To highlight its application for anticancer prodrug therapies, this study then utilized lectin-directed artificial metalloenzymes for the gold-catalyzed activation of an EBB-masked prodrug against targeted hypersialylated cancer cells.