O-(1，3-二芳硒基)异丙基-O-2-(N^3-替加氟)乙基硫代磷酯的合成及其抗癌活性

Synthesis of O-(1,3-diarylseleno)isopropyl-O-2-(N^3-tegafur) ethyl Thiophosphates and Their Antitumor Activities

六乙基亚磷酰三胺依次与羟乙基替加氟、1-芳硒基甘油及硫反应,得到环甘油硫代磷脂替加氟缀合物(2a^2 e);通过苯硒化钾对2进行亲核开环,得到O-(1,3-二芳硒基)异丙基-O-2-(N3-替加氟)乙基硫代磷酯(3a^3 e),其结构经1H NMR,31P NMR,MS及元素分析确证。3对膀胱癌细胞PGA1有一定的抑制作用。

Hexaethylphosphorous triamide reacted with N1 -（2-furanidyl）-N3- （hydroxyethyl）-5-fluyorouracil and 1-arylseleno glycerol as well as sulfur in one-pot to prepare intermediates 2a - 2e. 2a - 2e reacted with potassium phenylselenoate to give O-（ 1,3-diarylseleno） isopropyl-O-2-（N3-tegafur） ethyl thiophosphates（3a -3e）. The structures were confirmed by ^1H NMR, ^31p NMR, MS and elemental analysis. 3a - 3e showed antitumor activities against human urinary bladder cancer cell PGA1.