为了寻找结构新颖的生物活性分子,采用活性亚结构拼接原理设计合成了12个哌嗪取代呋喃查尔酮衍生物(3a ～31),其结构经1H NMR、13C NMR和HRMS确证.分别采用MTT法和小鼠巨噬细胞Raw264.7炎症模型对目标化合物的体外细胞毒活性和抗炎活性进行测试,结果表明,哌嗪环上的取代基对化合物的生物活性有明显的影响.特别是化合物3j和3k对肿瘤细胞株Hela和A549均表现出良好的体外抑制活性,而且化合物3d能有效抑制NO的生成,值得进一步研究.%In order to find new potent biological gents,twelve 4'-(N-substitued-l-piperazinyl) furanyl chalcone derivatives (3a ～31) are designed and synthesized by the general principle of molecular hybridization.The structures are charcterised by 1H NMR,13C NMR and HRMS.In vitro cytotoxic activities against a panel of human tumor cell lines (Hela,A549 and SGC7901) are tested by the MTT assay,and the anti-inflammatory activities in lipopolysaccharide (LPS)-Sfimulated RAW-264.7 macrophages are evaluated.The result indicate that the sulstituents of the NH group of piperasine ring have an obvious influence on biological activities.Especially,compounds 3i and 3k are found to be the potent compounds against Hela and A549,and compounds 3d has inhibitory effect on the generation of NO,which can be taken as lead compounds for further SAR research.
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