Design and Synthesis of Oligosaccharyltransferase Inhibitors: NGI-1 and Its Derivatives

Despite its proven efficacy and excellent as an OST inhibitor, the synthesis of NGI-1 (4) is poorly documented. In this study, we developed a robust synthetic protocol for NGI-1 and derivatives(4a-4j), featuring mild reaction conditions, scalability, and excellent yield and purity. Leveraging this methodology, we synthesized a series of derivatives(4a-4j) and subsequently evaluated their cytotoxicity against lung cancer cell lines A549. As consequence, compounds 4c, 4f, and 4j represent promising lead candidates, as their enhanced potency in suppressing cell viability outperforms that of the parent compound NGI-1. Additionally Simultaneously, all the compounds were unambiguously characterized by ¹H-NMR, ¹³C-NMR, and MS.

Publikationsverlauf

Eingereicht: 19. Januar 2026

Angenommen nach Revision: 11. Februar 2026

Accepted Manuscript online:
11. Februar 2026