Momparler R L, Momparler L F, Samson J
Leuk Res. 1984;8(6):1043-9. doi: 10.1016/0145-2126(84)90059-6.
The antineoplastic activity and effect on DNA synthesis and DNA methylation of 5-aza-2'-deoxycytidine (5-AZA-CdR), 1-beta-D-arabinofuranosylcytosine (ARA-C), and 5-azacytidine (5-AZA-CR) on L1210 leukemic cells were compared. At equimolar concentrations 5-AZA-CdR produced greater growth inhibition and more cytotoxicity against the L1210 cells than either ARA-C or 5-AZA-CR. ARA-C, but not 5-AZA-CdR or 5-AZA-CR, produced a potent inhibition of DNA synthesis in the L1210 cells. 5-AZA-CdR and 5-AZA-CR, but not ARA-C, inhibited DNA methylation with 5-AZA-CdR being a more effective inhibitor than 5-AZA-CR. At maximum tolerated dose, 5-AZA-CdR produced a much greater increase in life span of mice with L1210 leukemia than ARA-C or 5-AZA-CR. These in vitro and in vivo studies indicate that 5-AZA-CdR is a more potent antineoplastic agent against L1210 leukemic cells than either ARA-C or 5-AZA-CR.
比较了5-氮杂-2'-脱氧胞苷（5-AZA-CdR）、1-β-D-阿拉伯呋喃糖基胞嘧啶（ARA-C）和5-氮杂胞苷（5-AZA-CR）对L1210白血病细胞的抗肿瘤活性及其对DNA合成和DNA甲基化的影响。在等摩尔浓度下，5-AZA-CdR对L1210细胞产生的生长抑制作用和细胞毒性比ARA-C或5-AZA-CR更强。ARA-C能有效抑制L1210细胞中的DNA合成，但5-AZA-CdR和5-AZA-CR则不能。5-AZA-CdR和5-AZA-CR能抑制DNA甲基化，其中5-AZA-CdR的抑制效果比5-AZA-CR更显著，而ARA-C则无此作用。在最大耐受剂量下，5-AZA-CdR使L1210白血病小鼠的寿命延长幅度比ARA-C或5-AZA-CR大得多。这些体外和体内研究表明，相较于ARA-C或5-AZA-CR，5-AZA-CdR是一种对L1210白血病细胞更有效的抗肿瘤药物。
