3-苯甲酰基－2H-1-苯并吡喃－2-酮衍生物的设计、合成及抗肿瘤活性

Aim To design and synthesize 3-benzoyl-2H-1-benzopyran-2-one derivatives, and to assay their antitumor activities. Methods Substituted acetophenones were reacted with diethyl carbonate via Claisen condensation to obtain the corresponding β-keto esters, which were further treated with substituted salicylaldehydes through the Knoevenagel condensation and cyclization at the same time to yield the target compounds. The antitumor activities of some target compounds obtained were evaluated on the human acute promyelocy-tic leukemia cells HL-60 and the human breast cancer cells T47D in vitro. Results Eighteen compounds were obtained and thirteen of them were not reported in the literature, and their structures were characterized by 1H-NMR and IR. Among the compounds tested, compound Ⅲ15 showed good activity against T47D cells, with IC50 of 38 μmol•L^(-1);compounds Ⅲ1, Ⅲ2 and Ⅲ15 exhibited good activities against HL-60 cells, with IC50s of 37 μmol•L^(-1), 36 μmol•L^(-1) and 16 μmol•L^(-1) respectively. Conclusion The structure-activity relationships of 3-benzoyl-2H-1-benzopyran-2-one derivatives, as a novel type of tumor inhibitor, should be investigated furtherly.