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

作　　者：王世辉[1] 王岩[1] 朱玉莹[1] 韩健[1] 袁晓薇[1] Koirala Diwa 李大伟[2] 胡春[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]上海交通大学药学院,上海300193

出　　处：《中国药物化学杂志》2010年第5期342-347,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(40724053)

摘　　要：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.

关 键 词：化学合成 5H-呋喃并[3 2-g]色烯 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]