Kawaguchi T, Saito M, Saneyoshi M
Jpn J Cancer Res. 1986 May;77(5):436-9.
The antitumor effect of 5-fluoro-2'-deoxyuridine (FUdR) esters on L1210 in mice was enhanced by the simultaneous po administration of FUdR esters and acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil]-esters. Acyclothymidine (AcTdR), which strongly inhibits the phospholytic degradation of FUdR, was released from the AcTdR esters by enzymatic hydrolysis. The FUdR esters and AcTdR esters were found to be compatible in terms of their physicochemical properties and susceptibility to enzymatic hydrolysis.
5-氟-2'-脱氧尿苷(FUdR)酯与无环胸苷[5-甲基-1-(2'-羟基乙氧基甲基)尿嘧啶]酯同时经口给药,可增强其对小鼠L1210的抗肿瘤作用。无环胸苷(AcTdR)强烈抑制FUdR的磷酸解降解,通过酶促水解从AcTdR酯中释放出来。发现FUdR酯和AcTdR酯在物理化学性质和酶促水解敏感性方面是相容的。