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

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.