Hamamichi N, Miyasaka T
School of Pharmaceutical Science, Showa University, Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1992 Sep;40(9):2585-7. doi: 10.1248/cpb.40.2585.
The novel nucleosides 3-beta-D-ribofuranosylpyrazolo(3,2-i) purine (8) and their 9-substituted bromo, nitro and amino compounds (3, 6 and 11) have been prepared from a fully protected 3-beta-D-ribofuranosyl(3,2-i)purine-9-carboxyamide 1 by bromodeamidation (ipso bromination). Compounds 3, 8 and 11 exhibited antileukemic activity against mouse leukemia L5178Y cells in culture, while the 9-substituted nitro, ester and amide compounds (6, 12 and 13) showed no cytotoxicity.
新型核苷3-β-D-呋喃核糖基吡唑并(3,2-i)嘌呤(8)及其9-取代的溴代、硝基和氨基化合物(3、6和11)已通过脱酰胺溴化反应(本位溴化反应)，由完全保护的3-β-D-呋喃核糖基(3,2-i)嘌呤-9-甲酰胺1制备得到。化合物3、8和11在体外对小鼠白血病L5178Y细胞表现出抗白血病活性，而9-取代的硝基、酯和酰胺化合物(6、12和13)则无细胞毒性。
