四氢罂粟碱类似物的合成及活性评价  

Synthesis and Biological Evaluation of the Analogs of Tetrahydropapaverine

作　　者：冯德日 李林森[1] 金明林[1] 李丹妮[1] 

机构地区：[1]沈阳医学院,沈阳110034

出　　处：《科学技术与工程》2014年第26期1-4,12,共5页Science Technology and Engineering

摘　　要：以多种不同取代基苯甲酸为起始原料,经酰氯活化后与3,4-二甲氧基-β-苯乙胺盐酸盐在碱性条件下缩合,再经Bischler-Napieralski反应、NaBH4还原、成盐酸盐,最后得到8种四氢罂粟碱类似物,所有化合物之前均未见报道,结构经ESIMS和1H NMR确证。同时以α-那可丁为阳性对照药,进一步考察了目标化合物对U937白血病细胞、HL60人白细胞、HeLa人宫颈癌细胞等肿瘤细胞株增殖的抑制活性,结果表明部分目标化合物表现出了明显的抑制肿瘤细胞增殖活性。Different types of benzoic acid were activated by acyl chloride, condensed with 3,4-dihydroxymethylgroup-β-phenethylamines, followed by Bischler-Napieralski reaction with phosphorus oxychloride, then reducedwith NaBH4 and turned them into hydrochlorate to produce 8 different types of tetrahydropapaverine analogues final-ly. All the compounds were reported firstly, the structure of the target compounds were confirmed by means of ESI-MS and 1H NMR. It was found that some target compounds exhibited excellent inhibitory activity in the proliferationof U937, HL60 and HeLa cancer cell lines with β-Noscapine as positive control drug in the pharmacological tests.

关 键 词：四氢罂粟碱类似物 肿瘤 生物活性评价 

分 类 号：O626.3[理学—有机化学]