Inhibition of thymidine phosphorylase by 6-aminothymine and derivatives of 6-aminouracil.
Inhibition of thymidine phosphorylase by 6-aminothymine and derivatives of 6-aminouracil.
复制标题
6-氨基胸腺嘧啶和 6-氨基尿嘧啶衍生物对胸苷磷酸化酶的抑制作用。
DOI：
10.1016/0006-2952(67)90260-2
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发表时间：
1967
影响因子：
5.8
通讯作者：
B. Preussel
中科院分区：
文献类型：
--
作者：
P. Langen;G. Etzold;D. Bärwolff;B. Preussel
胸腺嘧啶和 5-溴-、5-碘-和 5-氟尿嘧啶的 6-氨基取代衍生物是胸苷磷酸化酶的体外强效抑制剂； 6-肼基-胸腺嘧啶，特别是6-叠氮胸腺嘧啶的活性明显较低。 6-氨基取代的衍生物的抑制作用似乎是基于由胸腺嘧啶和5-卤代尿嘧啶引起的该酶的产物抑制的强化。 6-氨基取代使这些化合物的抑制特性增强 2 至 9 倍。鉴于在人体内5-氟脱氧尿苷和5-碘脱氧尿苷被胸苷磷酸化酶快速转化为无活性产物（5-碘尿嘧啶）或毒性更大的产物（5-氟尿嘧啶）的事实，预计所描述的抑制剂类型具有实际重要性。
6-Aminosubstituted derivatives of thymine and of 5-bromo-, 5-iodo- and 5-fluorouracil are powerful inhibitorsin vitroof thymidine phosphorylase; 6-hydrazino-thymine and, particularly, 6-azidothymine are significantly less active. The inhibitory action of the 6-aminosubstituted derivatives seems to be based on a fortification of the product inhibition of this enzyme brought about by thymine and the 5-halogenated uracils. 6-Aminosubstitution enhances 2- to 9-fold the inhibitory properties of these compounds. In view of the fact that in man 5-fluorodeoxyuridine and 5-iododeoxyuridine are rapidly converted by thymidine phosphorylase into an inactive product (5-iodo-uracil) or more toxic product (5-fluorouracil), the type of inhibitors described may be expected to be of practical importance.