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本文设计合成了系列新型4-取代-3-硝基苯甲酰胺类化合物,并通过1H NMR、13C NMR、MS及元素分析确证了目标化合物的结构。以HCT-116、MDA-MB435及HL-60三种细胞株为活性筛选对象,利用SRB法进行初步体外抗肿瘤活性研究。结果表明,大部分化合物对于所试验的癌细胞的增殖都有一定程度的抑制作用,其中化合物4a对3种癌细胞的抗增殖作用最显著,GI50为1.904~2.111μmol·L-1;化合物4g、4l~4n对MDA-MB435和HL-60的抑制活性较强,其GI50值分别为1.008~3.586μmol·L-1和1.993~3.778μmol·L-1,在此基础上初步探讨了此类化合物的构效关系。
In this paper, a series of novel 4-substituted-3-nitrobenzamides were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR, MS and elemental analysis. The three cell lines HCT-116, MDA-MB435 and HL-60 were screened for activity and SRB method was used to study the antitumor activity in vitro. The results showed that most of the compounds inhibited the proliferation of the tested cancer cells to a certain extent. Among them, compound 4a exhibited the most significant antiproliferative effect on three kinds of cancer cells with a GI50 of 1.904-2.1111μmol·L-1. Compound 4g , 4l ~ 4n had stronger inhibitory activity on MDA-MB435 and HL-60, and their GI50 values were 1.008 ~ 3.586μmol·L-1 and 1.993 ~ 3.778μmol·L-1, respectively. On this basis, Structure-activity relationship of compounds.