| 摘要 |
The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-alpha (TNF-alpha). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-alpha. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-kappaB or GSK-3beta activation or NF-kappaB activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.
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