Matthes E, Reimer K, von Janta-Lipinski M, Meisel H, Lehmann C
Institut für Molekularbiologie, Humboldt-Universität Berlin (Charité), Germany.
Antimicrob Agents Chemother. 1991 Jun;35(6):1254-7. doi: 10.1128/AAC.35.6.1254.
Of a series of 14 nucleoside 5'-triphosphates, those of 2',3'-dideoxy-3'-fluoro-5-methylcytidine, 3'-azido-2',3'-dideoxy-5-methylcytidine, 2',3'-dideoxy-3'-fluoroguanosine, 2',3'-didehydro-2',3'-dideoxy-5-methylcytidine, 2',3'-dideoxy-3'-fluoro-5-ethylcytidine, and 2',3'-dideoxy-3'-fluoroadenosine emerged as the most potent inhibitors of hepatitis B virus DNA polymerase (50% inhibitory dose, 0.03 to 0.35 microM). In contrast, cellular DNA polymerases proved to be resistant to (alpha) or partially affected by (beta) these analogs. These compounds are among the most effective and selective inhibitors of endogenous hepatitis B virus DNA polymerase recognized to date.
在一系列14种核苷5'-三磷酸中，2',3'-二脱氧-3'-氟-5-甲基胞苷、3'-叠氮基-2',3'-二脱氧-5-甲基胞苷、2',3'-二脱氧-3'-氟鸟苷、2',3'-二脱氢-2',3'-二脱氧-5-甲基胞苷、2',3'-二脱氧-3'-氟-5-乙基胞苷和2',3'-二脱氧-3'-氟腺苷的核苷5'-三磷酸表现为乙型肝炎病毒DNA聚合酶的最有效抑制剂（半数抑制剂量，0.03至0.35微摩尔）。相比之下，细胞DNA聚合酶被证明对这些类似物具有抗性（α）或受到部分影响（β）。这些化合物是迄今为止公认的内源性乙型肝炎病毒DNA聚合酶最有效和最具选择性的抑制剂之一。
