摘要
以鱼藤酮为原料经3步反应合成鱼藤素;鱼藤素分别经三溴化硼脱甲基和硼氢化钠还原合成了4个新型含游离羟基的鱼藤素衍生物(3a^3c和4),其结构经1H NMR,13C NMR和LC-MS表征。初步的抗肿瘤活性测定结果表明,12-羟基鱼藤素(4)对人乳腺癌细胞MCF-7和人肺癌细胞H299的抑制活性较好,其IC50分别为0.11μmol·L-1和0.01μmol·L-1,优于阳性对照药Deguelin。
Deguelin was prepared by three-step reaction from Rotenone. Novel deguelin derivatives containing free hydroxyl groups（ 3a ~ 3c and 4） were synthesized by boron tribromide demethylation or reduction with sodium cyanoborohydride from deguelin. The structures were characterized by1 H NMR,13 C NMR and LC-MS. The antitumor activities were investigated. The results showed that12-hydroxyl deguelin（ 4） showed the best inhibition activities against MCF-7 and H1299 with IC50of0. 11 μmol·L-1and 0. 01 μmol·L-1,respectively,which was better than deguelin.
出处
《合成化学》
CAS
CSCD
2015年第11期1013-1016,1021,共5页
Chinese Journal of Synthetic Chemistry
基金
广东省重大科技专项[广东医院制剂研究开发技术平台建设(2011A080300004)]
关键词
鱼藤酮
鱼藤素衍生物
合成
抗肿瘤活性
rotenone
deguelin derivative
synthesis
antitumor activity
