Nagai K, Yokoyama S, Kawai G, Shuhadlnik R J, Takaku H
Department of Industrial Chemistry, Chiba Institute of Technology, Japan.
Nucleic Acids Symp Ser. 1990(22):13-4.
The 8-(2-hydroxypropyl)-adenosine and 8-hydroxy adenosine-substituted analogues of 2-5A and it's derivatives were synthesized and their biological activity was evaluated in mouse L cell extracts. The 8-hydroxy adenosine-substituted analogues (i.e. pppAOH2'p5AOH2'p5'AOH, pAOH2'p5'AOH2'p5'AOH, pppA2'p5'A2'p5'AOH, pA2'p5'A2'p5'AOH) inhibited protein synthesis with a relative activity compared to the parent 2-5A. Further, the greater interest is the observation that the corresponding 5'-monophosphate had to inhibitory activity. However, 8-(2-hydroxypropyl)-adenosine substituted analogue (pAHPr2'p5'AHPr2'p5'AHPr) can not about bound as well as parent 2-5A.
合成了2-5A及其衍生物的8-(2-羟丙基)-腺苷和8-羟基腺苷取代类似物，并在小鼠L细胞提取物中评估了它们的生物活性。8-羟基腺苷取代类似物（即pppAOH2'p5AOH2'p5'AOH、pAOH2'p5'AOH2'p5'AOH、pppA2'p5'A2'p5'AOH、pA2'p5'A2'p5'AOH）与母体2-5A相比，以相对活性抑制蛋白质合成。此外，更值得关注的是相应的5'-单磷酸酯没有抑制活性这一观察结果。然而，8-(2-羟丙基)-腺苷取代类似物（pAHPr2'p5'AHPr2'p5'AHPr）与母体2-5A相比结合不佳。
