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目的：研究一系列３（Ｒ）单脱氧异核苷的合成和抗肿瘤活性。方法和结果：由Ｌ木糖出发，合成了环氧化物５（Ｒ）二甲氧甲基３（Ｓ），４（Ｓ）环氧四氢呋喃４；在碱性条件下，利用嘌呤的Ｎ９位或嘧啶的Ｎ１位对环氧化物进行亲核进攻，得到一系列３（Ｒ）单脱氧异核苷５ａｄ和６ａｄ；并进行了体外抗肿瘤活性筛选。结论：其中３（Ｒ）单脱氧异核苷５ａｄ为首次报道；同已报道的３（Ｓ）单脱氧异核苷合成方法相比，路线缩短，收率提高。在体外抗肿瘤和端粒酶抑制活性筛选中，只有化合物６ａ显示了对ＢＩＵ细胞较弱的抑制活性，其余均未显示有意义的抗肿瘤活性和端粒酶抑制活性。
Objective: To study the synthesis and antitumor activities of a series of 3 (R) monodeoxyoxynucleosides. Methods and Results: Starting from L-xylose, epoxides 5 (R) dimethoxymethyl 3 (S) and 4 (S) tetrahydrofuran 4 were synthesized. Under alkaline conditions, Purine N9 or pyrimidine N1 position on the nucleophilic attack of epoxides to obtain a series of 3 (R) monoxygenucleosides 5a d and 6ad; and in vitro anti-tumor activity screening. Conclusions: Among them, 3 (R )monooxyonucleoside 5ad was reported for the first time. Compared with the reported 3 (S )monooxyisonosine synthesis method, the route was shortened and the yield was increased. Of the in vitro anti-tumor and telomerase inhibitory activity screens, only compound 6a showed weaker inhibitory activity against BIU cells, and none showed significant anti-tumor activity and telomerase inhibitory activity.