摘要
以齐墩果酸(oleanolic acid,OA)为先导化合物进行结构修饰,通过对A环进行开环改造,28位酰胺结合,设计并合成了4个未见文献报道的化合物(Ⅰ1~Ⅰ4).目标产物结构通过1H-NMR确认,对所合成的目标化合物以人肺癌细胞(A549)和人胃癌细胞(SGC7901)进行体外抗肿瘤活性测试.结果表明:目标化合物对两种肿瘤细胞的抑制活性均明显强于OA;化合物Ⅰ4对A549细胞显示出较强活性(IC_(50)=13.3μmol·L^(-1)).
With oleanolic acid(OA)as the lead compound,four compounds were designed and synthesized by ring-opening modification of A ring and 28-position amide binding.The structure of the target product was confirmed by 1H-NMR.The antitumor activities of the synthesized compounds in human lung cancer cells(A549)and human gastric cancer cells(SGC7901)was tested in vitro.The results showed that the inhibitory activity of the target compound on both tumor cells was significantly stronger than that of OA.The results showed that compoundⅠ4 exhibited stronger inhibitory activity against A549 cells(IC_(50)=13.3μmol·L^(-1)).
作者
张蓬勃
宋艳玲
ZHANG Peng-bo;SONG Yan-ling(Shenyang University of Chemical Technology,Shenyang 110142,China)
出处
《沈阳化工大学学报》
CAS
2021年第1期25-29,共5页
Journal of Shenyang University of Chemical Technology
基金
辽宁省自然科学基金项目资助(2015020687)。
关键词
齐墩果酸衍生物
合成
抗肿瘤活性
oleanolic acid derivatives
synthesis
antineoplastic activity
作者简介
张蓬勃(1994-),男,河北石家庄人,硕士研究生在读,主要从事新药研发;通信联系人:宋艳玲(1977-),女,吉林通化人,副教授,博士,主要从事新药研发.
