Empetrifranzinans A和Empetrifranzinans C的全合成及其抗肿瘤活性  

Total Synthesis and Antitumor Activities of Empetrifranzinans A and Empetrifranzinans C

作　　者：李人则 刘晓宇[1] 焦晓臻[1] 田承森 董梁[1] 谢平[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所天然药物活性物质与功能国家重点实验室活性物质发现与适药化研究北京市重点实验室,北京100050

出　　处：《合成化学》2013年第4期461-464,共4页Chinese Journal of Synthetic Chemistry

摘　　要：以间苯三酚为起始原料,L-脯氨酸为催化剂,经由两步反应首次合成了Empetrifranzinans A(1a,总收率60%)和Empetrifranzinans C(总收率55%),其结构经1H NMR,13C NMR和HR-MS确证。初步药理筛选实验结果表明,1a对人结肠癌、肝癌、胃癌、肺腺癌、卵巢癌细胞表现出了较强的细胞毒作用,其IC50分别为<0.1,1.31,4.90,8.98和3.65μmol·L-1。Empetrifranzinans A（1a） and Empetrifranzinans C were firstly synthesized by proline-catalysed condensation between phloroglucinol and citral in the total yield of 60% and 55%,respectively.The structures were confirmed by 1H NMR,13C NMR and HR-MS.Preliminary antitumor activities test indicated that 1a exhibited potent antitumor activities against human coloniccarcinoma,hepatocellular carcinoma,gastric carcinoma,lugh adenocarcinoma epithelial and ovarian cancer cell line,IC50 were 0.1,1.31,4.90,8.98 and 3.65 μmol·L-1,respectively.

关 键 词：脯氨酸 Empetrifranzinans A Empetrifranzinans C 合成 抗肿瘤活性 

分 类 号：O625.31[理学—有机化学]