Momparler R L, Momparler L F, Samson J
Int J Cancer. 1982 Sep 15;30(3):361-64. doi: 10.1002/ijc.2910300317.
The in vitro and in vivo antineoplastic activity of 5-AZA-2'-deoxycytidine (5-AZA-CdR) and beta-2'-deoxythioguanosine (TGdR) on L1210 and L1210/ARA-C (resistant to cytosine arabinoside) leukemic cells was investigated. 5-AZA-CdR was a very potent cytotoxic agent against the L1210 leukemia cells. This analogue was inactive against L1210/ARA-C leukemic cells because these cells lack deoxycytidine kinase, the enzyme that converts 5-AZA-CdR to its active nucleotide form. TGdR was a potent cytotoxic agent to both L1210 and L1210/ARA-C leukemic cells. In mice which were injected simultaneously with both L1210 and L1210/ARA-C leukemic cells, the drug combination of 5-AZA-CdR plus TGdR had a very potent antineoplastic activity and produced long-term survivors. Either agent alone did not produce any long-term survivors in the mice with L1210 and L1210/ARA-C leukemia. This experimental model indicates that 5-AZA-CdR plus TGdR is an interesting drug combination for the treatment of leukemia with drug-resistant cells.
研究了5-氮杂-2'-脱氧胞苷（5-AZA-CdR）和β-2'-脱氧硫代鸟苷（TGdR）对L1210和L1210/ARA-C（对阿糖胞苷耐药）白血病细胞的体外和体内抗肿瘤活性。5-AZA-CdR是一种对L1210白血病细胞非常有效的细胞毒剂。该类似物对L1210/ARA-C白血病细胞无活性，因为这些细胞缺乏脱氧胞苷激酶，即一种将5-AZA-CdR转化为其活性核苷酸形式的酶。TGdR对L1210和L1210/ARA-C白血病细胞均为有效的细胞毒剂。在同时注射L1210和L1210/ARA-C白血病细胞的小鼠中，5-AZA-CdR加TGdR的药物组合具有非常强的抗肿瘤活性，并产生了长期存活者。单独使用任何一种药物在患有L1210和L1210/ARA-C白血病的小鼠中均未产生任何长期存活者。该实验模型表明，5-AZA-CdR加TGdR是一种用于治疗具有耐药细胞的白血病的有趣药物组合。
