5H-呋喃并[3,2-g]色烯类化合物的合成及其抗肿瘤活性

Synthesis and antitumor activity of 5H-furo [3,2-g] chromen derivatives

目的设计合成5H-呋喃并[3,2-g]色烯类化合物,并测定其体外抗肿瘤活性。方法以2′,4′-二羟基苯乙酮为原料,经缩合、催化氢化和Fries重排等反应合成目标化合物。采用人骨肉瘤细胞U2OS-EGFP-4A12G对目标化合物的体外抗肿瘤活性进行初步评价。结果与结论合成了10个未见文献报道的5H-呋喃并[3,2-g]色烯类化合物,其结构经红外光谱、质谱、核磁共振氢谱确证。化合物7a、7e和7h对人骨肉瘤细胞U2OS-EGFP-4A12G的抑制活性较强,其IC50值分别为16.53、7.74、13.27μmol.L-1。5H-呋喃并[3,2-g]色烯类化合物是一类具有新型骨架结构的抗肿瘤化合物,值得进一步研究。

Aim To design and synthesize a series of 5H-furo[3,2-g]chromen derivatives,and to evaluate their antitumor activity.Methods The target compounds were synthesized from 2′,4′-dihydroxyacetophenone via condensation,catalytic hydrogenation and Fries rearrangement,etc.The antitumor activities of the target compounds obtained were evaluated on human osteosarcoma cell U2OS-EGFP-4A12G in vitro.Results and conclusion Ten 5H-furo[3,2-g]chromen derivatives were synthesized and all of them were not reported in li-terature,and their structures were characterized by IR,MS,and 1H-NMR.Compounds 7a,7e and 7h showed good activity on U2OS-EGFP-4A12G cells in vitro,with the IC50s of 16.53 μmol·L-1,7.74 μmol·L-1 and 13.27 μmol·L-1,respectively.5H-Furo[3,2-g]chromen derivatives,as new antitumor agents with novel scaffold,could be investigated in the further.