School of Pharmaceutical Science, Zhengzhou University, Ke Xue Da Dao 100, Zhengzhou 450001, PR China.
Steroids. 2010 Jun;75(6):419-23. doi: 10.1016/j.steroids.2010.02.007. Epub 2010 Feb 18.
A series of digoxin derivatives containing the gamma-alkylidene butenolide moiety were synthesised by way of stereoselective vinylogous aldol reaction of the unactivated butenolide in simple conditions. The structures of compounds synthesised were characterised by infrared (IR), nuclear magnetic resonance (NMR) and HR-MS. Preliminary bioassay shows that some of them have cardiac functions, especially compound 2g that induced a marked increase in myocardial contractility at 10ngml(-1) and 20ngml(-1) concentrations without digitalis toxicity.
一系列含有γ-亚烷基丁烯内酯部分的洋地黄毒苷衍生物是通过在简单条件下未活化的丁烯内酯的立体选择性 vinylogous aldol 反应合成的。所合成的化合物的结构通过红外（IR）、核磁共振（NMR）和高分辨率质谱（HR-MS）进行了表征。初步的生物测定表明，其中一些具有心脏功能，特别是化合物 2g，在 10ngml(-1) 和 20ngml(-1)浓度下没有洋地黄毒性，明显增加了心肌收缩力。
