Concise syntheses of selective inhibitors against α-1,3-galactosyltransferase.
Concise syntheses of selective inhibitors against α-1,3-galactosyltransferase.
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DOI：
10.1039/c0ob00042f
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发表时间：
2010-10
影响因子：
3.2
通讯作者：
Guo-Liang Zhang;Li-he Zhang;X. Ye
中科院分区：
文献类型：
--
作者：
Guo-Liang Zhang;Li-he Zhang;X. Ye
以简明的路线设计和合成了几个基于亚氨糖的尿苷二磷酸半乳糖模拟化合物1-4，包括d-和L-同分异构体，并在体外评价了这些化合物对α-1，3-和β-1，4-半乳糖基转移酶的抑制作用。实验结果表明，L-差向异构体2对α-1，3-半乳糖基转移酶的抑制活性最强，选择性中等。
Several iminosugar-based uridine diphosphate galactose (UDP-Gal) mimetics 1-4 including d- and l-epimers were designed and synthesized by concise routes, and these synthetic compounds were evaluated for the inhibition of α-1,3- and β-1,4-galactosyltransferases in vitro. The experimental data demonstrated that l-epimer 2 displayed the strongest inhibitory activity with moderate selectivity against α-1,3-galactosyltransferase.