Sharma Vasudha, Lansdell Theresa A, Jin Guangyi, Tepe Jetze J
Department of Chemistry, Michigan State University, East Lansing, MI 48824, USA.
J Med Chem. 2004 Jul 1;47(14):3700-3. doi: 10.1021/jm040013d.
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 (IC(50) = 2.4 microM) and tumor necrosis factor alpha (IC(50) = 1.4 microM) production. One of the hymenialdisine derived indoloazepines was found to also inhibit interleukin-2 (IC(50) = 3.5 microM) and tumor necrosis factor alpha (IC(50) = 8.2 microM) production.
我们在此描述了两种与海洋海绵代谢产物膜海鞘素结构相关的吲哚氮杂卓的合成及其生物活性。天然产物膜海鞘素被发现是白细胞介素-2（IC50 = 2.4微摩尔）和肿瘤坏死因子α（IC50 = 1.4微摩尔）产生的有效抑制剂。其中一种源自膜海鞘素的吲哚氮杂卓也被发现能抑制白细胞介素-2（IC50 = 3.5微摩尔）和肿瘤坏死因子α（IC50 = 8.2微摩尔）的产生。
