抗瘤酮A_(10)类似物的合成及抗癌作用  

Synthesis and Antitumour Activity of Antineoplaston A_(10) Derivatives

作　　者：王福兰[1] 戴华成[1] 王央贡[1] 舒平 管见 

机构地区：[1]同济医科大学药学系有机药物化学教研室

出　　处：《同济医科大学学报》1993年第2期101-102,共2页Acta Universitatis Medicinae Tongji

摘　　要：抗瘤酮A_(10)是从人尿中提取的内源性抗癌物质,具有抗瘤谱广、低毒、刺激提高免疫力的特点。本文采用酸醉交换法、L-谷氨酰胺法,合成抗瘤酮A_(10)的 4个类似物,即:①3-苯甲酰胺基2,6-哌啶二酮;②4-甲氧基3-苯甲酰胺基2,6-哌啶二酮;③3-苯丙酰胺基 2,6-哌啶二酮;④4-甲氧基3-苯乙酰胺基2,6-哌啶二酮。并通过对艾氏(EAC)腹水癌体外抗癌活性试验,显示类似物3、4具有明显的抗癌作用。Four Antineoplaston A10 derivatives (3-benzoyl amino-piperidi-ne-2,6-dione, 3-(4-methoxybenzoyrl)-amino-piperidine-2,6-dione, 3-phenylpro-pionyl-amino-piperidine-2,6-dione, and 3-phenylacetyl-amino-piperidine-2,6-dione) were synthesized by two methods (acetic anhydride exchanging method and L-glut-amine method). The inhibitory activity (Ehrlich ascitic cancer cell) of the derivatives was measured. The resurts show that compound 3 and compound 4 have significant anticancer activity.

关 键 词：抗瘤酮A10 类似物 抗癌药 合成 

分 类 号：TQ463.24[化学工程—制药化工]