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Simplified Sialyl Lewisx Analogues with Improved E-Selectin Inhibition

التفاصيل البيبلوغرافية
العنوان: Simplified Sialyl Lewisx Analogues with Improved E-Selectin Inhibition
المؤلفون: Thoma, Gebhard, Schwarzenbach, Franz
المصدر: Helvetica Chimica Acta; March 2003, Vol. 86 Issue: 3 p855-864, 10p
مستخلص: The simplified sialyl Lewisx mimic 5 containing a D-arabinose, a 3-cyclohexyl-2-hydroxypropanoate, and a tetrahydropyran building block instead of L-fucose, sialic acid, and N-acetylglucosamine, respectively was synthesized. Compound 5 was 10-fold more potent than sLex in a static E-selectin binding assay and showed at 50 μM 75% inhibition in a dynamic-flow assay in which sLex did not inhibit neutrophil rolling at up to 1000 μM. Compound 7 with a lactic acid instead of sialic acid building block showed threefold improved potency compared to sLex.
قاعدة البيانات: Supplemental Index
الوصف
تدمد:0018019X
15222675
DOI:10.1002/hlca.200390085