论文部分内容阅读
为寻找高效、低毒的抗肿瘤候选化合物,以1-杂环取代-β-咔啉-3-羧酸乙酯为原料,合成了一系列的双-(1-杂环-β-咔啉)-3-烷氨基衍生物.所有目标化合物经请下载后查看，本文暂不支持在线获取查看简介。1H NMR、~(13)C NMR和HRMS进行结构确证.以顺铂为阳性对照药,采用四甲基偶氮唑盐(MTT)法考察了目标化合物体外抗肿瘤(22RV1,SK-OV-3,MCF-7,BGC-823,A375和769-P等10株细胞)活性.结果显示化合物5a~5h与阳性对照药和单取代β-咔啉衍生物相比具有很好的抗肿瘤活性,其IC_(50)值均小于10μmol·L~(-1),特别是化合物5d对769-P的抑制活性达到0.8μmol·L~(-1),化合物5h对22RV1的抑制活性达到0.6μmol·L~(-1).
In order to find efficient and low toxicity anti-tumor candidate compounds, a series of bis- (1-hepto-β-carboline ) -3-alkylamino derivatives. All target compounds are available after download. This article does not support the online introduction. 1H NMR, ~ (13) C NMR and HRMS.The anti-tumor activity of the target compounds in vitro (22RV1, SK-OV-3 , MCF-7, BGC-823, A375 and 769-P, etc. The results showed that the compounds 5a ~ 5h had good antitumor activity compared with the positive control and the monosubstituted β-carboline derivatives, The IC 50 values were less than 10 μmol·L -1. Especially, the inhibitory activity of compound 5d on 769-P reached 0.8 μmol·L -1. The inhibitory activity of compound 5h on 22RV1 reached 0.6 μmol·L -1 L ~ (-1).