Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1344-6. doi: 10.1016/j.bmcl.2010.01.018. Epub 2010 Jan 11.
The 70% aqueous methanolic extract of the Chinese plant Aristolochia manshuriensis was found to contain two novel substituted phenanthrene compounds, SCH 546909 (1), and another phenanthrene glycoside (2). The structures of 1 and 2 were established based on NMR studies. They were identified as inhibitors of the CDK2 enzyme. Compound 1 was found to be a potent inhibitor of the CDK2 enzyme with an IC50 of 140 nM, whereas compound 2 was found to be less active with an IC50 of >10 microM.
从中国植物东北马兜铃中提取的 70%甲醇水溶液中发现了两种新型取代菲类化合物 SCH 546909(1)和另一种菲类糖苷(2)。根据 NMR 研究确定了 1 和 2 的结构。它们被鉴定为 CDK2 酶的抑制剂。化合物 1 被发现是一种有效的 CDK2 酶抑制剂,IC50 为 140 nM,而化合物 2 的活性较低,IC50 大于 10 microM。