查尔酮衍生物的合成及抗增殖活性的研究

Synthesis and Anti-proliferation Activity Evaluation of Chalcone Derivatives

将查尔酮做为先导化合物,以苯乙酮和对甲基苯乙酮为原料和对苯二甲醛进行克莱森-施密特羟醛缩合反应,并在另一端引入氨基胍,或用一锅法将原料两端的醛基同时取代,最终得到一系列查尔酮衍生物结构的衍生物。采用MTT检测目标化合物体外抗肿瘤活性。目标化合物结构经^(1)H-NMR、^(13)C-NMR及MS确证。活性结果显示,目标化合物对于肿瘤细胞产生一定的抗肿瘤活性。该类型查尔酮衍生物结构具有一定抑制肿瘤细胞的活性,值得进一步研究。

The target compound was prepared with chalcone as the lead compound.Acetophenone and p-methylacetophenonewere usedas raw materials to carry out Claisen-Schmidt condensation for tereph tha laldehyde.Afterintroducingaminoguanidine at the other end,or using a one-pot method to simultaneously replace the aldehyde groups at both ends of the raw material,a series of chalcone derivativeswere obtained.MTT was used to detect the in vitro antitumor activity of the target compound.The structure of the target compound was confirmed by ^(1)H-NMR,^(13)C-NMR and MS.In vitro anti-tumor results showed that the target compound had certain anti-tumor activity on cells.The chalconederived structure of this type had certain antitumor activity on tumor cells,which was worthy of further study.