Yu H W, Zhang L R, Zhou J C, Ma L T, Zhang L H
School of Pharmaceutical Sciences, Beijing Medical University, People's Republic of China.
Bioorg Med Chem. 1996 Apr;4(4):609-14. doi: 10.1016/0968-0896(96)00048-x.
A series of 4'-(R)-hydroxy-5'-(S)-hydroxymethyl-tetrahydrofuranyl purines and pyrimidines were synthesized by the reaction of 3,4-epoxy-5-(S,trans)-dimethoxymethyl-tetrahydrofuran and nucleobases under the catalysis of potassium tert-butoxide and 18-crown-6. Compounds 6a, 6c and 7b have shown significant inhibition on the growth of HL-60 cells. The phosphotriester and phosphodiester of isonucleoside 8a-d were synthesized and cytotoxic activities were reported. The conformation of isonucleosides in solution was studied by 1H NMR.
通过3,4-环氧-5-(S,反式)-二甲氧基甲基-四氢呋喃与核苷酸碱基在叔丁醇钾和18-冠-6催化下反应，合成了一系列4'-(R)-羟基-5'-(S)-羟甲基-四氢呋喃基嘌呤和嘧啶。化合物6a、6c和7b对HL-60细胞的生长表现出显著抑制作用。合成了异核苷8a-d的磷酸三酯和磷酸二酯，并报道了其细胞毒性活性。通过1H NMR研究了溶液中异核苷的构象。
