N′-叔丁氨基羰基-N-(5-取代苯基-2-呋喃甲酰基)硫脲的合成及对白血病K562细胞增殖的影响  

Synthesis and Inhibition of N′-Tertbutylaminocarbonyl-N-5-Substitutedphenyl-2-furylformylthiourea Derivatives Against K562 Cell Proliferation

作　　者：蔡志娟[1] 薛思佳[1] 申杰峰[1] 王庆东[1] 

机构地区：[1]上海师范大学生命与环境科学学院,上海200234

出　　处：《应用化学》2008年第5期552-555,共4页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金(20672073);上海市重点学科建设项目(T0402)资助项目

摘　　要：将活性基团5-取代苯基呋喃环和叔丁氨基引入酰基硫脲的分子骨架中,设计合成了8个未见文献报道的N′-叔丁氨基羰基-N-(5-取代苯基-2-呋喃甲酰基)硫脲类化合物(5a^5h),结构经元素分析、IR和1HNMR等测试技术得到确证。经MTT(溴化3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑)法观察,首次发现目标化合物对白血病K562细胞的增殖有明显的抑制作用。在药物浓度为100×10-6g/mL时,大部分目标化合物对白血病K562细胞生长的抑制率超过了70%,化合物5a对白血病K562细胞生长的抑制率达到77.14%。其中,目标化合物5f和5h对白血病K562细胞有诱导作用,进一步的测试正在进行中。Eight novel N′-tertbutylaminocarbonyl-N-5-substitutedphenyl-2-furylformylthiourea derivatives were synthesized by taking active group 5-substitutedphenyl furan and tert-butylamino into the acylthiourea. Their structures were elucidated and confirmed by elemental analysis, IR, and ^1H NMR. The inhibitory rate of cellular growth of K562 ceils was measured via MTT assay. The results indicated that the title compounds have some effects on the cellular growth inhibition to K562 ceils of leukemia.

关 键 词：合成 N′-叔丁氨基羰基-N-(取代苯基呋喃甲酰基)硫脲 MTT法 白血病K562细胞 

分 类 号：O622[理学—有机化学]