Development of novel glycolipids that activates lymphocytes to induce anticancer activity

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KRN7000, an alpha-galactosylated sphingolipid, stimulates natural killer T cells to induce antitumor activity. Based on the X-ray crystallographic analysis of CD1d/KRN7000/TCR, structure-activity relationship study on the 6-hydroxyl group of the galactose part of KRN7000 was performed. We synthesized several 6’’-carbamate analogs of KRN7000. It was found that these analogs were potent immunostimulants, and induced a large amount of IFN-gamma production in vivo (mouse).