Bobek M, Cheng Y C, Mihich E, Bloch A
Recent Results Cancer Res. 1980;74:78-83. doi: 10.1007/978-3-642-81488-4_11.
Various 2'-azido- and 2'-aminoarabinofuranosyl purine and pyrimidine nucleosides have been synthesized. Among these, the derivatives of cytosine and of adenine inhibit the growth of some tumor cell lines in vitro and in vivo. 2'-Azidoarabinofuranosyl cytosine also interferes with the replication of herpes simplex virus types I and II. Whereas 2'-azidoara-C is resistant to deamination by a partially purified CdR deaminase from KB cells, the adenine derivatives are substrates for aminohydrolases partially purified from calf and mouse intestines. Both azido- and aminoara-C are phosphorylated by partially purified CdR kinases from leukemia L1210 and from human AML blast cells. The accumulated data encourage exploration of the clinical utility of the more potent of these analogues.
已经合成了多种2'-叠氮基和2'-氨基阿拉伯呋喃糖基嘌呤和嘧啶核苷。其中，胞嘧啶和腺嘌呤的衍生物在体外和体内均能抑制某些肿瘤细胞系的生长。2'-叠氮基阿拉伯呋喃糖基胞嘧啶也会干扰I型和II型单纯疱疹病毒的复制。虽然2'-叠氮基阿糖胞苷对来自KB细胞的部分纯化的胞苷脱氨酶的脱氨作用具有抗性，但腺嘌呤衍生物是从小牛和小鼠肠道中部分纯化的氨基水解酶的底物。叠氮基阿糖胞苷和氨基阿糖胞苷都能被来自白血病L1210和人急性髓性白血病母细胞的部分纯化的胞苷激酶磷酸化。积累的数据鼓励探索这些类似物中更有效的药物的临床应用。
