摘要/Abstract

喹啉类衍生物、芳腙以及酰腙类化合物都具有显著的生物活性，以1-萘胺、取代苯甲醛和丙酮酸甲酯为起始原料经Doebner-Miller反应生成苯并[h]喹啉甲酸甲酯，酯还原后再氧化得到相应的醛.取代苯并[h]喹啉甲醛分别与肼盐和酰肼反应合成苯并[h]喹啉腙及酰腙类化合物.初步活性数据表明大部分化合物对细胞周期分裂蛋白25B（CDC 25B）和蛋白酪氨酸磷酸酶PTP 1B表现出较显著的抑制活性.
关键词: 苯并[h]喹啉衍生物, 腙, 酰腙, CDC 25B, PTP 1B, 抑制活性
Quinoline derivatives, aryl hydrazines and hydrazide compounds have significant biological activities. Benzo[h] quinoline derivatives were synthesized from 1-naphthylamine, substituted benzaldehyde and methyl pyruvate by Doebner-Miller reaction. After the ester was reduced, the corresponding aldehyde was obtained by oxidation. Benzo[h] quinolinium and quinoline hydrazide compounds were synthesized by reacting benzo[h] quinoline formaldehyde with hydrazine salts and hydrazides, respectively. The preliminary activity data showed that most of the compounds exhibited significant inhibitory activities against cycle protein 25B (CDC 25B) and protein tyrosine phosphatase PTP 1B.
Key words: Benzo[h]quinoline derivatives, hydrazone, hydrazide, CDC 25B, PTP 1B, inhibitory activity


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