Synthesis and immunosuppressive activity of new artemisinin derivatives containing polyethylene glycol group

AimTo search for new artemisinin derivatives with higher immunosuppressive activity. MethodsTwo 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. ConclusionThese 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.