Van Calenbergh S, Link A, Kunick C, Herdewijn P
Faculteit Farmaceutische Wetenschappen, Universiteit Gent, Belgium.
Pharmazie. 1999 Oct;54(10):727-9.
With focus on exploring the structural demands of adenosine triphosphate pockets of different target enzymes, the 3'-amido-3'-deoxyadenosines 1-7 were synthesized. The inhibitory activity of these compounds on a selected cyclin-dependent kinase as model target in anticancer research was evaluated in vitro. A starfish oocyte enzyme based assay revealed a decreased inhibitory activity in comparison to adenosine. Consequently, the introduction of spacefilling lipophilic 3'-amido substituents alters the enzyme inhibition in an unfavorable manner.
着眼于探索不同靶酶三磷酸腺苷口袋的结构要求，合成了3'-氨基-3'-脱氧腺苷1-7。在体外评估了这些化合物对作为抗癌研究中模型靶标的一种选定细胞周期蛋白依赖性激酶的抑制活性。一种基于海星卵母细胞酶的测定显示，与腺苷相比，其抑制活性降低。因此，引入空间填充亲脂性3'-氨基取代基以不利的方式改变了酶抑制作用。
