摘要
目的合成系列新型苯基呋喃-2甲-酮类化合物,测定其体外血清诱导血管平滑肌细胞(VSMC)增殖抑制活性并初步探讨其构效关系。方法以取代苯甲酸和呋喃甲酸为原料,经多步反应制得目标化合物,通过标准胚胎血清(FBS)诱导的VSMC增殖模型测定化合物抑制VSMC增殖活性。结果与结论合成了18个化合物,其中9个为未见文献报道的新化合物,其结构经ESI-MS、1H-NMR、13C-NMR确证,总收率70%～95%。体外活性实验表明,18个目标化合物中,有15个在质量浓度为5.0μg.mL-1时有一定的抑制活性,其中新化合物7b、11a及化合物3 c表现出较强的抑制活性,新化合物11a的IC50值为2.52μg.mL-1。
A series of new（furan-2-yl）（phenyl）methanones were synthesized,their inhibitory activities against vascular smooth muscle cells（VSMC） proliferation in vitro along with the preliminary SAR were investigated.（Furan-2-yl）（phenyl）methanone derivatives were prepared from benzoic acids or furan-2-carboxylic acid,followed by chlorination,Friedel-Crafts reaction and demethylation.Eighteen target compounds were prepared by this simple and mild route with total yields from 70% to 95%,among them nine are new derivatives,their structures were confirmed by 1H-NMR,13C-NMR and ESI-MS.The VSMC inhibitory activi-ties of the target compounds were evaluated.Some new compounds showed potential in vitro activity.The results showed that fifteen target compounds exhibited inhibitory activity at 5.0 μg·mL-1.The new compounds 7b,11a and compound 3c showed strong inhibitory activity,the IC50 value of the new compound 11a is 2.52 μg·mL-1.
出处
《中国药物化学杂志》
CAS
CSCD
2011年第4期256-261,共6页
Chinese Journal of Medicinal Chemistry
基金
"重大新药创制"科技重大专项(2009ZX09302-003)
北京大学天然药物与仿生药物国家重点实验室资助项目(20080210)
山西省留学归国人员基金资助项目(2008-51)
