摘要/Abstract

为了寻找高效低毒的抗肿瘤药物，设计并合成了一系列新型的含N-（3-丙烯酰胺苯基）乙酰胺结构的喹唑啉类衍生物，并采用噻唑蓝（MTT）法测定了目标化合物对H1975（人肺腺癌细胞系），PC-3（人前列腺癌细胞系），MGC-803（人胃癌细胞系）三种肿瘤细胞的抗增殖活性.结果显示大部分化合物具有较好的抗肿瘤活性，其中N-（3-（2-（（（4-（（4-氯苯基）氨基）-7-甲氧基喹唑啉-6-基）氧基）乙酰氨基）苯基）丙烯酰胺（13j）对H1975，MGC-803两种细胞显示出最好的抗增殖活性，IC₅₀值分别为（6.77±0.65）和（4.06±0.34）μmol/L，其活性均优于阳性对照品吉非替尼，为抗肿瘤药物的研究提供了线索.
关键词: 丙烯酰胺, 喹唑啉, 合成, 抗肿瘤活性
In order to find efficient and low toxicity anti-tumor drugs, a series of novel quinazoline derivatives containing N-(3-aminophenyl)acrylamide were synthesized and their antiproliferative activities were evaluated against three human cancer cell lines (H1975, PC-3, MGC-803) by using methyl thiazolyl tetrazolium (MTT) assay. The results showed that most compounds exhibited better antiproliferative activities against the four human tumor cell lines. Among them, N-(3-(2-((4-((4-chlorophenyl)amino)-7-methoxy-quinazolin-6-yl)oxy)acetamido)phenyl)acrylamide (13j) showed the best antiproliferative activity against H1975 and MGC-803 cancer cell lines with IC₅₀ values of (6.77±0.65) and (4.06±0.34) μmol/L, respectively. Its activity was better than the positive control gefitinib. In a nutshell, this work provides clues to discover antitumor agent based on the quinazoline scaffold.
Key words: acrylamide, quinazoline, synthesis, antiproliferative activity


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