Antileukemic Activities and Mechanism of Action of 2′-Deoxy-4′-methylcytidine and Related Nucleosides
Antileukemic Activities and Mechanism of Action of 2′-Deoxy-4′-methylcytidine and Related Nucleosides
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2′-脱氧-4′-甲基胞苷及相关核苷的抗白血病活性及作用机制
DOI：
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发表时间：
1997
期刊：
影响因子：
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通讯作者：
M. Saneyoshi
中科院分区：
文献类型：
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作者：
Toyofumi Yamaguchi;A. Tomikawa;T. Hirai;T. Kawaguchi;H. Ohrui;M. Saneyoshi
摘要研究了几种含2‘-脱氧-4’-甲基胞苷类似物及其Arac类似物对小鼠白血病P388细胞的体内外抗白血病活性。两种化合物在体外均表现出明显的细胞抑制活性(IC_(50)=0.4μM)，而前者以3 mg/kg/d×5的剂量给药，在体内表现出较高的活性(T/C=175%)。对这些5‘-三磷酸对DNA聚合酶的作用机理也作了详细的阐述。
Abstract Antileukemic activity of several analogues containing 2′-deoxy-4′-methylcytidine and its araC counterpart were evaluated against murine leukemic P388 cells in vitro and in vivo. Both compounds showed significant cytostatic activity (both IC50=0.4 μM) in vitro and the former compound administered intraperitoneally at a dose of 3 mg/kg/day × 5 showed high activity (T/C=175%) in vivo. The mechanism of action of these 5′-triphosphates on DNA polymerases in detail will be also described.