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Synthesis, biological evaluation of chrysin derivatives as potential immunosuppressive agents

European Journal of Medicinal Chemistry, ISSN: 0223-5234, Vol: 46, Issue: 1, Page: 393-398
2011
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Article Description

A series of novel chrysin derivatives was firstly synthesized and evaluated on their immunosuppressive activity in the search for potential immunosuppressive agents. Among them, compounds 5c displayed the most potent immunosuppressive inhibitory activity with IC 50 of 0.78 μM, which was comparable to that of cyclosporin A (IC 50  = 0.06 μM). The preliminary mechanism of compound 5c inhibition effects was also detected by flow cytometry (FCM), and the compound exerted immunosuppressive activity via inducing the apoptosis of activated lymph node cells in a dose dependent manner. Furthermore, the estimated LD 50 (in mg/kg) in vivo of compound 5c is 738.2, which indicated that compound 5c was low toxic.

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