新型4-(5-N-取代-1,3,4-噻二唑-2-巯基)-苯并4,5呋喃3,2-d嘧啶类衍生物的合成及其抗癌活性

摘要

Ten new 4-(5-N-substituted-l,3,4-thiadiazole-2-thiol)ben2o[4,5]furo[3,2-d]pyrimidine derivatives(3a ~3j) were designed and synthesized by 5-substituted-amido-2-thiol-l ,3,4-thiadiazole into benzo[4,5]furo[3,2-d]pyrimidine. The structures were characterized by 1H NMR, 13C NMR, IR and MS. Preliminary bioassay tests indicates that 3a ~ 3j possess antitumor activity to MGC cells in vitro by MTT method. The antiproliferation activity of 4-(5-/V-2'-methoxylphenyl-l ,3 ,4-thiadiazole-2-ylthio)benzo[4,5]furo[3,2-rf]pyrimidine(3j) to MGC cells was 86.4% at the 10 jxmol ? IT1.%将5-取代胺基-2-巯基-1,3,4-噻二唑引入苯并[4,5]呋喃[3,2-d]嘧啶中,设计并合成了10个新型的4-(5-N-取代-1,3,4-噻二唑-2-巯基)-苯并[4,5]呋喃[3,2-d]嘧啶类衍生物(3a～3j),其结构经1H NMR,13C NMR,IR和MS确认.用MTT法测定了3a～3j对人胃腺癌细胞体(MGC)的体外增殖活性.结果表明,3a～3j均具有不同程度的抑制MGC的活性,其中4-(5-N-2′-甲氧基苯基-1,3,4-噻二唑-2-巯基)-苯并[4,5]呋喃[3,2-d]嘧啶(3j)在10 μmol·L-1的浓度下对MGC的抑制率为86.4％.