A series of oxime ester-derivatives were prepared by utilizing the schizandrin (1), a major compound isolated from Schisandra grandiflora, which is deployed in different traditional system of medicine. The in vitro antiproliferative activities of the synthesized compounds were assessed against a selected panel of human cancer cell lines (A549, RKO P3, DU145 and Hela) and normal cell (HEK293). Several of these derivatives were found more potent in comparison to parent compound, schizandrin (1). Particularly, 4a and 4b demonstrated potent activity against DU-145 and RKOP3 cell lines with IC₅₀ values of 3.42 µM and 3.35 µM respectively. To characterize the molecular mechanisms involved in antitumoral activity, these two compounds, 4a and 4b were selected for further studies. Cell cycle analysis revealed that both the compounds were able to induce apoptosis and cell cycle arrest at G₀/G₁ phase. To know the extent of apoptosis in DU145 and RKOP3 cell lines, Annexin V-FITC were performed. Moreover, the tubulin polymerization assay indicated that 4a and 4b exhibits potent inhibitory effect on the tubulin assembly. Molecular docking studies and competitive binding assay also indicated that 4a and 4b effectively bind at the colchicine binding site of the tubulin.

利用五味子醇（1）制备了一系列肟酯衍生物，五味子醇是从五味子中分离出的主要化合物，并被部署在不同的传统医学系统中。在体外合成的化合物的抗增殖活性进行了评估针对人类肿瘤细胞系（A549，RKO P3，DU145和Hela）和正常细胞（HEK293）中所选择的面板。与母体化合物五味子素（5）相比，发现这些衍生物中的几种更有效。特别是，图4a和图4b显示了具有IC _50的针对DU-145和RKOP3细胞系的有效活性值分别为3.42 µM和3.35 µM。为了表征参与抗肿瘤活性的分子机制，选择了这两种化合物4a和4b进行进一步研究。细胞周期分析显示这两种化合物均能够诱导细胞凋亡和细胞周期停滞在G ₀ / G ₁期。为了知道DU145和RKOP3细胞系中的细胞凋亡程度，进行了膜联蛋白V-FITC。此外，微管蛋白聚合测定表明4a和4b对微管蛋白组装体表现出有效的抑制作用。分子对接研究和竞争性结合测定还表明4a和4b在微管蛋白的秋水仙碱结合位点有效结合。