Studies on the stereoselective synthesis and immunosuppressive activity of dihydroartemisinin-O-glycoside derivatives. Issue 16 (15th August 2020)

• Record Type: Journal Article
• Authors: Yu, Yu; Yu, Jingfeng; Zou, Xiaosu; Xu, Wei; Zhang, Jinghua; Bian, Hongzhu; Dong, Xun; Shen, Zhengwu
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 16(2020)
• Publication Date: 2020-08-15
• Subjects: Dihydroartemisinin -- Glycoside -- Immunosuppressive; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.127338
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Eight new dihydroartemisinin-O-glycosides were synthesized with their relative configurations were determined based on NMR spectrum. In vitro immunosuppressive assay showed that 10α-dihydroartemisinin-β-O-d -mannoside (19a) demonstrate 88% inhibition towards T cells proliferation and 98% reduction in IFN-γ levels in cell media. These results suggest that dihydroartemisinin-O-glycoside as a potential lead for further in vivo evaluation.