2-溴-4-[1-(E)-亚乙基-2-对甲氧基苯基-丁基]-1-甲氧基苯脱甲基及双键转位反应的研究

2-溴-4-1-(E)-亚乙基-2-对甲氧基苯基-丁基]-1-甲氧基苯(3)是在合成3’-甲氧基己烯雌酚(2)过程中获得的意外羟基消除产物. 报道了2-溴-4-1-(E)-亚乙基-2-对甲氧基苯基-丁基]-1-甲氧基苯在不同条件下的脱甲基反应产物以及双键转位反应的情况. 部分重要中间体的人脐静脉内皮细胞(HUVEC)抑制活性结果显示, 己烯雌酚骨架上的基团对该类化合物的抑制新生血管生成活性具有显著的影响, 甲氧基为活性有利基团, 而酚羟基全部游离时化合物没有活性.

Demethylation and Double-Bond Isomerisation of 2-Bromo-4-[1-eth- (E)-ylidene-2-(4-methoxy-phenyl)-butyl]-1-methoxy-benzene

Some different demethylation products and the double bond isomer of 2-bromo-4-1-eth-(E)- ylidene-2-(4-methoxy-phenyl)-butyl]-1-methoxy-benzene (3) were obtained under different conditions dur-ing synthesizing 3’-methoxyl-1,2-diethystilbestrol (2). The angiogenesis inhibitory activities of some com-pounds were evaluated on human umbilical vein endothelial cells and the assay data indicated that the groups substituted on the skeleton of diethystilbestrol analogs could significantly affect their anti-angiogenesis activities.