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为了寻找高效低毒的抗肿瘤候选化合物,我们对β-咔啉环的1,2,9三个结构位点进行了设计与合成,得到了一系列的1-取代-β-咔啉衍生物,这些化合物的结构经~1H NMR、~(13)C NMR、MS、IR及元素分析确证。采用四甲基偶氮唑盐(MTT)法考察了目标化合物体外抗肿瘤(Bel-7402,HepG2,A549,A375,786-0和HT-29)活性,构效关系结果显示β-咔啉1位取代基团对抗肿瘤活性的影响趋势为:2-噻吩基>2-氯苯基>4-氯苯基>苄基。
In order to find efficient and low toxicity anti-tumor candidate compounds, we design and synthesize the three structural sites of 1, 2 and 9 of β-carboline ring and get a series of 1-substituted-β-carboline derivatives The structures of these compounds were confirmed by ~ 1H NMR, ~ (13) C NMR, MS, IR and elemental analysis. The antitumor activity of the target compounds (Bel-7402, HepG2, A549, A375, 786-0 and HT-29) in vitro was investigated by MTT assay. The structure-activity relationship results showed that β-carboline 1 The influence of substituent on the antitumor activity tended to be: 2-thienyl> 2-chlorophenyl> 4-chlorophenyl> benzyl.