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根据恩其明(ungeremine,1.)分子中存在次甲基N-O-O三角和内铵盐结构,这可能和其抗肿瘤活性有密切关系的设想,合成了它的开环类似物2-羟基-8,9-次甲二氧基菲啶溴甲(或乙)烷季铵盐(3a和3b)和2-羟基-8,9-二甲氧基菲啶甲(或乙)烷季铵盐(4a和4b)等有关化合物,作为抗肿瘤作用的比较,以探讨恩其明的构效关系。 动物试验表明:化合物3a对小鼠艾氏腹水癌有明显抑制作用,小鼠生命时间延长130～140％,其它化合物则无明显活性。
According to the presence of methylated NOO triglycine and betaine in the ungeremine (1) molecule, which may be closely related to its anti-tumor activity, its open-loop analogue 2-hydroxy-8 , 9-methoxyphenanthridine bromide (or ethane) quaternary ammonium salts (3a and 3b) and 2-hydroxy-8,9-dimethoxyphenanthramine (or ethane) quaternary ammonium salt 4a and 4b) and other related compounds, as a comparison of antitumor effects to explore the structure-activity relationship of enqimine. Animal experiments show that: compound 3a has obvious inhibitory effect on Ehrlich ascites carcinoma in mice, the life span of mice is prolonged by 130-140%, while the other compounds have no obvious activity.