Synthesis and Potent Antileukemic Activities of N-Lactylsphingosine and N-Lactyldihydrosphingosine

N-(R)- and N-(S)-Lactylsphingosine and their corresponding dihydrosphingosine derivatives were synthesized. The antileukemic activities of these compounds were measured by MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) assay in human leukemia HL-60 cells. N-(R)- and N-(S)-Lac...

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Veröffentlicht in:Journal of medicinal chemistry 2003-07, Vol.46 (16), p.3445-3447
Hauptverfasser: Azuma, Hideki, Takao, Ryoko, Shikata, Keiji, Niiro, Hayato, Tachibana, Taro, Ogino, Kenji
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Sprache:eng
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Zusammenfassung:N-(R)- and N-(S)-Lactylsphingosine and their corresponding dihydrosphingosine derivatives were synthesized. The antileukemic activities of these compounds were measured by MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) assay in human leukemia HL-60 cells. N-(R)- and N-(S)-Lactylsphingosine displayed higher activities than N-acetylsphingosine (C2-ceramide, a well-known apoptosis inducer), and their dihydrosphingosine derivatives had slight activities.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm030125p