1,2,3,4-四氢喹啉衍生物的合成与抗癌活性评价  

Synthesis and preliminary evaluation of 1,2,3,4-tetrahydroquinoline derivatives as potent anticancer reagents

作　　者：赵敏[1] 樊维[1] 李杰[1] 海俐[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2011年第4期316-318,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的设计并合成了10个不同氨基取代的呋喃或吡喃并四氢喹啉衍生物,并探讨其抗癌活性。方法以对氯硝基苯为原料,经过乌尔曼偶联、脱甲基、还原、氮杂-DA反应等方法合成了目标物并进行了抗癌活性的初筛。结果与结论目标化合物及重要中间体经1HNMR、MS等确证;化合物Ⅰ1、Ⅰ7及Ⅰ9显示了较好的抗癌活性。OBJECTIVE To synthesize 10 aryl amine substituted furano-or pyranoquinoline derivatives,and evaluate their anticancer activities.METHODS The target compounds were synthesized from p-chloronitrobenzene through Ullmann coupling reaction,demethylation,reduction and aza-Diels-Alder reaction,and the preliminary anticancer activity test was carried out.RESULTS and CONCLUSION The chemical structure of the target compounds and key intermediates were characterized by their respective 1HNMR and MS.The evaluation in vitro showed that compounds Ⅰ1,Ⅰ7 and Ⅰ9 exhibited asignificant anticancer activity.

关 键 词：合成 DA反应 1 2 3 4-四氢喹啉衍生物 抗癌活性 

分 类 号：R914[医药卫生—药物化学] R06[医药卫生—药学]