Synthesis and Evaluation of 1,2,3-Triazole Containing Analogues of the Immunostimulant -GalCer

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• 作者：Taeho Lee ; Minjae Cho ; Sung-Youl Ko ; Hyun-Jun Youn ; Dong Jae Baek ; Won-Jea Cho ; Chang-Yuil Kang ; Sanghee Kim
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：February 8, 2007
• 年：2007
• 卷：50
• 期：3
• 页码：585 - 589
• 全文大小：140K
• 年卷期：v.50,no.3(February 8, 2007)
• ISSN：1520-4804

文摘

-GalCer is the first defined and most potent agonistic antigen of the T cell receptor of natural killer Tcells. We have prepared a series of 1,2,3-triazole-containing -GalCer analogues in which the lipid chainlengths have been incrementally varied. We found that this isosteric replacement of -GalCer's amide moietywith triazole increases the IL-4 versus IFN- bias of released cytokines. The stimulatory effect was influencedby the length of the attached chain. In particular, the long-chained triazole analogues have a comparablestimulatory effect on cytokine production as -GalCer and exhibit a stronger Th2 cytokine response.