3-苯甲酰基香豆素的合成及抗肿瘤活性研究

Synthesis and antitumor activity study of 3-benzoylcoumarins

以4-甲基哌啶为催化剂,取代的苯甲酰乙酸乙酯与取代的水杨醛类化合物在甲醇中环合,合成了21个3-苯甲酰基衍生物1-21,其中15个为新化合物。所有化合物经重结晶或硅胶柱分离纯化,得到纯度较高的目标产物并经^(13)C NMR、^(1)H NMR和ESI-MS确证。采用MTT法检测其对人肺癌H1299细胞株的抗癌活性,并以常用的抗肿瘤药物拓扑替康(Topotecan,TPT)作为对照药物。化合物2对H1299细胞具有较强的生长抑制活性,IC_(50)=9.151±0.669μmol·L^(-1),小于拓扑替康的IC_(50)值(16.053±0.750μmol·L^(-1))。

Twenty-one 3-benzoyl coumarins 1-21 were synthesized by cyclization reactions of substituted ethylbenzoylacetates and salicylaldehydes catalyzed by 4-methylpiperidine in methanol,15 of which are new compounds.All the compounds were purified by recrystallization or silica gel column to obtain higher purity,and confirmed by ^(13)C NMR、^(1)H NMR and ESI-MS.MTT assay was used to assess the anticancer activity of the compounds against human lung cancer H1299 cell line,and Topotecan(TPT),a commonly used antitumor drug,was used as the control.Compound 2 shows strong growth inhibition activity against H1299 cells with IC_(50)=9.151±0.669μmol·L^(-1),which is lower than that of topotecan(16.053±0.750μmol·L^(-1)).