β-榄香烯胺类衍生物的合成及抗癌活性研究  

Synthesis and anti-proliferative activity of β-elemene amino derivatives

作　　者：徐莉英[1] 王宪明[2] 于志瀛[2] 董金华[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2009年第4期247-250,260,共5页Chinese Journal of Medicinal Chemistry

基　　金：辽宁省教育厅创新团队基金项目(2007T176)

摘　　要：目的合成β-榄香烯胺类衍生物,并对其体外抗癌活性进行初步的评价。方法β-榄香烯经氯代、胺化制备目标化合物。以SRB法测试目标化合物对HL-60、HeLa、SGC-7901细胞的增殖抑制活性。结果与结论合成了12个新化合物,其结构经IR、MS和1H-NMR确证。初步药理结果显示大部分目标化合物的体外抗癌活性明显强于β-榄香烯。Aim To synthesize novel β-elemene amino derivatives and to test their in vitro antitumor activi- ties. Methods The target compounds were synthesized from β-elemene via chlorination and sequential amination. The in vitro anti-proliferative effects of the target compounds on HL-60, HeLa and SGC-7901 cells were evaluated by SRB assay. Results and conclusion The structures of 12 novel compounds were characterized by IR, MS and ^1H-NMR. Preliminary pharmacological results showed that most compounds possessed stronger antitumor activities than β-elemene.

关 键 词：体外抗癌活性 Β-榄香烯 衍生物 合成 胺类 SGC-7901细胞 ^1H-NMR 新化合物 

分 类 号：R914[医药卫生—药物化学] R730.5[医药卫生—药学]