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4,5-Cis Unsaturated α‑GalCer Analogues Distinctly Lead to CD1d-Mediated Th1-Biased NKT Cell Responses

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journal contribution
posted on 15.06.2015, 00:00 by Yanli Cui, Zhiyuan Li, Zhaodong Cheng, Chengfeng Xia, Yongmin Zhang
The total synthesis of 4,5-cis unsaturated α-GalCer analogues was achieved, and their immune-response altering activity was assessed in vitro as well as in vivo in mice. Using glycosyl iodide as a glycosyl donor, construction of the sphingosine unit was shortened by four steps and single α-stereoselectivity was achieved in good yield (67%). With regard to the therapeutic use of α-GalCer, the novel analogues (1b and 1c) distinctly induced a Th1-biased cytokine response, avoiding induction of a contradictory response and overstimulation.