Donghi Monica, Attenni Barbara, Gardelli Cristina, Marco Annalise Di, Fiore Fabrizio, Giuliano Claudio, Laufer Ralph, Leone Joseph F, Pucci Vincenzo, Rowley Michael, Narjes Frank
Department of Medicinal Chemistry, IRBM-MRL Rome, Via Pontina Km 30,600, 00040 Pomezia (Rome), Italy.
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1392-5. doi: 10.1016/j.bmcl.2009.01.035. Epub 2009 Jan 19.
A variety of new prodrugs of 2'-methyl cytidine based on acyloxy ethylamino phosphoramidates have been synthesized and tested in vitro and in vivo for their biological activity. Compared with the parent drug a 10- to 20-fold increase in formation of nucleotide triphosphate in rat and human hepatocytes could be achieved.
已经合成了多种基于酰氧基乙氨基磷酸酯的2'-甲基胞苷前药，并在体外和体内对其生物活性进行了测试。与母体药物相比，在大鼠和人肝细胞中三磷酸核苷酸的形成可增加10至20倍。
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