新地钱素A的合成及抗肿瘤活性  

Synthesis and Antitumor Activity of Neomarchantin A

作　　者：刘德秀[1] 王延风[2] 黄晓英[1] 潘华英[1] 

机构地区：[1]苏州卫生职业技术学院药学院,江苏苏州215009 [2]山东省医学科学院药物所,山东济南250000

出　　处：《化学试剂》2016年第1期22-26,62,共6页Chemical Reagents

基　　金：江苏省卫生厅科研资助项目(JZ201422)

摘　　要：以香兰素、异香兰素、间溴苯甲醛和对溴苯甲酸甲酯为原料,通过Ullmann反应、醛基与酚羟基的保护和脱保护、醛基还原、磷盐生成、Wittig反应以及烯烃的催化氢化反应等方法完成了新地钱素A的全合成。所得化合物的结构通过MS、~1HNMR进行确证。采用MTT法测试目标化合物体外抗肿瘤（A549、MCF-7、U20S）活性。结果表明,新地钱素A对A549和MCF-7表现出较好的抑制活性。Neomarchantin A was totally synthesized from vanillin,isovanillin,3-bromobenzaldehyde and methyl 4-bromobenzoate,through Ullmann reaction,aldehyde group and phenolic hydroxyl protection and de-protection,aldehyde group reduction,phosphorus salt formation,Witting reaction,catalytic hydrogenation of alkene reaction. The structure was confirmed by MS and1 HNMR.Antitumor effect in vitro activity（ A549,MCF-7 and U2OS） was tested by MTT method and the result shows that Neomarchantin A has a good inhibitory activity for A549 and MCF-7.

关 键 词：新地钱素A 合成 抗肿瘤活性 

分 类 号：R914.5[医药卫生—药物化学]