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Inhibition of Cytokine Production by Hymenialdisine Derivatives

2004; American Chemical Society; Volume: 47; Issue: 14 Linguagem: Inglês

10.1021/jm040013d

1520-4804

Vasudha Sharma, Theresa A. Lansdell, Guangyi Jin, Jetze J. Tepe,

Chemical Synthesis and Analysis

We describe herein the synthesis and biological activity of two indoloazepines that are structurally related to the marine sponge metabolite hymenialdisine. The natural product hymenialdisine was found to be a potent inhibitor of interleukin-2 (IC50 = 2.4 μM) and tumor necrosis factor α (IC50 = 1.4 μM) production. One of the hymenialdisine derived indoloazepines was found to also inhibit interleukin-2 (IC50 = 3.5 μM) and tumor necrosis factor α (IC50 = 8.2 μM) production.