含硒的替加氟硫代磷酯合成

Synthesis of tegafur sulfurphospholopid containing selenium

目的:合成含硒的替加氟的硫代磷酯,并测定其活性。方法:2-N,N-二乙胺基-1,3,2-二氧磷杂戊烷依次与羟乙基替加氟及硫反应,得到中间体2-O-(N^1-替加氟)乙基-3-S-1,3,2-二氧磷杂戊烷(2)。化合物2与芳硒化钠反应得到标题化合物3。结果:得到3个新化合物,其结构经过~1H NMR,^(31)P NMR及MS确证。试验了3a～c对膀胱癌细胞T-24、胃癌细胞BGC-823抑制作用。结论:化合物3a～3c对膀胱癌细胞T-24和胃癌细胞BGC-823具有一定的抑制作用。

Objective ： To investigate the synthesis and bioactive assay of tegafur sulfurphospholopid containing selenium. Methods： 2-N,N-diethylamino-1,3,2-dioxaphsopholane was reacted with N^1- （2-furanidyl） -N3- （hydroxyethyl） -5-fluyorouracil and sulfur to give intermediates 2-0-（ N3 -2-tegafur） eth- yl-3-S-1,3,2-dioxaphsopholane （2）. （2） was reacted with ArSeNa to give the target compounds. Results： Three new compounds have been synthesized. Their structure were confirmed by ^1H NMR,^31P NMR and MS. The antitumor activity was investigated. Conclusion：The title compounds had good antitumor activity against bladder cancer cell T-24 and stomach cancer cell BGC-823.