- 作者: 李榮展,張凱宣,劉行讓,李文山
- 作者服務機構: Institute of Chemistry, Academia Sinica, Taipei 115, Taiwan, R.O.C.
- 中文摘要: The first series of 5'-triazole cytidines 1a-d and adenosines 2a-c was prepared and evaluated for inhibitory potency toward a-2,3-sialyltransferase. The synthesis of target compounds was achieved by converting the 5'-alcohol of protected nucleosides to the azide derivatives, which were then coupled with the alkynes by copper(I)-catalyzed cycloaddition to give protected 5'-triazole nucleosides 3a-d/7a-c, followed by deprotection. 5'-Triazole adenosines 2a-c were less efficient inhibitors of a-2,3-sialyltransferase than their cytidine analogues 1a-d. 1d was the most active compound with an IC50 of 37.5 μM. These results suggested that the hydrophobic functionality and the cytidine group are clearly required for the improved binding.
- 英文摘要: --
- 中文關鍵字: α-2,3-Sialyltransferase; 5'-Triazole nucleosides; Click chemistry; Inhibitory assay; Structure-based drug design approach.
- 英文關鍵字: --