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DOI: 10.1055/a-2811-7374
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Design and Synthesis of Oligosaccharyltransferase Inhibitors: NGI-1 and Its Derivatives

Authors

  • Lixin Wang

    1   College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, China (Ringgold ID: RIN66280)

  • Yan Jin 

    1   College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, China (Ringgold ID: RIN66280)

  • Peijun Yin

    2   Qingdao Customs Technology Center, Technology Center of Qingdao Customs, Qingdao, China (Ringgold ID: RIN674420)

  • Yiqi Li

    1   College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, China (Ringgold ID: RIN66280)
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Graphical Abstract

Abstract

Despite its proven efficacy and excellent as an oligosaccharyltransferase 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 a 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, all compounds were unambiguously characterized by 1H NMR, 13C NMR, and MS.

Keywords

NGI-1 - Synthesis - Derivatives - Process optimization - Antitumor activity

Supplementary Material



Publication History

Received: 19 January 2026

Accepted after revision: 11 February 2026

Accepted Manuscript online:
11 February 2026

Article published online:
27 February 2026

© 2026. Thieme. All rights reserved.

Georg Thieme Verlag KG
Oswald-Hesse-Straße 50, 70469 Stuttgart, Germany

 

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