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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。
Objective To design and synthesize 5H-furo [3,2-g] chromene compounds and determine their anti-tumor activity in vitro. Methods The target compounds were synthesized from 2 ’, 4’-dihydroxyacetophenone by condensation, catalytic hydrogenation and Fries rearrangement. In vitro anti-tumor activity of the target compound was evaluated using human osteosarcoma cell line U2OS-EGFP-4A12G. RESULTS AND CONCLUSION Ten novel 5H-furo [3,2-g] chromene compounds were synthesized. Their structures were confirmed by IR, MS and 1H-NMR. The inhibitory activity of compounds 7a, 7e and 7h on human osteosarcoma cells U2OS-EGFP-4A12G was stronger with IC50 values of 16.53, 7.74 and 13.27μmol.L-1.5H-furo [3,2-g] Analogs are a class of antitumor compounds with novel scaffolds and deserve further study.