芹菜素衍生物的合成及抗肿瘤活性研究

Synthesis and Antitumor Activity of Apigenin Derivatives

以芹菜素为起始原料,在C-5、C-6、C-7、C-4′位置上引入甲基、苄基、乙酰基、对甲苯磺酰基、三异丙基硅烷基等多种单元结构基团,合成了16个芹菜素衍生物,采用CCK-8的方法考察了所合成化合物对人肝癌细胞(Hep3β)、人结肠癌细胞(LOVO)、人肺癌细胞(A549)的抑制作用。结果显示,经过化学修饰后的部分化合物比芹菜素有更强的抗肿瘤活性,其中化合物13对人肺癌细胞(A549)的抑制率超过了顺铂,值得进一步探讨和研究。

Using apigenin as starting material,a series of apigenin derivatives were synthesized by introducing methyl,benzyl,acetyl,p-toluenesulfonyl and triisopropyl silyl groups at C-5,C-6,C-7 and C-4′positions.The inhibitory effects of the synthesized compounds on human hepatoma cells(Hep3β),human colon cancer cells(LOVO)and human lung cancer cells(A549)were investigated by CCK-8 assay.The results showed that some modified compounds display stronger anti-tumor activity than apigenin.Especially,compound 13 exhibites more excellent inhibitory rate on human lung cancer cells(A549)than that of cisplatin,which is worthy of further exploration.