Department of Chemistry, Hunan University of Science and Engineering, Yongzhou 425100, PR China.
Eur J Med Chem. 2009 Nov;44(11):4716-20. doi: 10.1016/j.ejmech.2009.05.030. Epub 2009 Jun 6.
A series of D-glucopyranosyl-1,2,4-triazole-3-thione derivatives 1a-1d were synthesized by the reaction of 1,2,4-triazole-3-thione Schiff bases 5a-5d with 2,3,4,6-tetra-O-acetyl-sigma-D-glucopyranosyl bromide. We demonstrate the conversion of 2 to 5, without the necessity of purification of both oxadiazole and triazole intermediates to afford the compounds 5. Their structures were confirmed by standard studies of (1)H NMR, IR, MS and elemental analysis. Analogues 5 and 1 have shown cytotoxic activity against human MCF-7 and Bel-7402 malignant cell lines.
一系列 D-葡萄糖基-1,2,4-三唑-3-硫酮衍生物 1a-1d 通过 1,2,4-三唑-3-硫酮席夫碱 5a-5d 与 2,3,4,6-四-O-乙酰-sigma-D-葡萄糖基溴反应合成。我们证明了 2 到 5 的转化，无需对恶二唑和三唑中间体进行纯化即可得到化合物 5。它们的结构通过（1）H NMR、IR、MS 和元素分析的标准研究得到证实。类似物 5 和 1 对人 MCF-7 和 Bel-7402 恶性细胞系表现出细胞毒性活性。
