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Updated: Aug 8, 2026
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
[Synthesis and immunosuppressive activity of new artemisinin derivatives containing polyethylene glycol group]
Jian-Xin Zhang1, Jun-Xia Wang, Yu Zhang
1Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Aim:
To search for new artemisinin derivatives with higher immunosuppressive activity.
Methods:
Two kinds of new artemisinin derivatives containing polyethylene glycol group were synthesized from dihydroartemisinin via condensation and esterification. These compounds were assayed for their inhibitory activity on ConA-induced T cell proliferation and LPS-induced B cell proliferation.
Results:
Twenty three new compounds (2a - 2f, 3a - 3d, 4a - 4f, 6a, 6b and 7a - 7g) were synthesized and identified by 1H NMR and elemental analysis.
Conclusion:
These compounds had immunosuppressive activity in vitro. Among them, the symmetrical substituted compound 2 and 6 had higher activity than mono-substituted compound 3, 4 and 7. Especially, compounds 2a - 2f remarkably exhibited higher inhibition in comparison with artemisinin and artesunate.
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