摘要
以齐墩果酸为先导化合物,在C-2位引入活性基团,并在C-28位引入胍基结构,设计并合成了一系列具有一定抗肿瘤活性的齐墩果酸类似物.使用MTT方法,选择人肺癌细胞(A549)和人胃癌细胞(SGC7901)对获得的化合物进行初步的体外抗肿瘤活性测试.筛选5种同一骨架的新型候选化合物,并通过_(1)H-NMR和^(13)C-NMR证实了其结构.结果表明:所测试的化合物对A549和SGC7901肿瘤细胞的抑制作用高于母体齐墩果酸,尤其是化合物R_(4)具有显著的抗肿瘤活性.
A series of oleanolic acid analogues with certain antitumor activity were designed and synthesized by using oleanolic acid as the lead compound,introducing active group at C-2 position and guanidine structure at C-28 position.Human lung cancer cells(A549)and human gastric cancer cells(SGC7901)were selected by MTT method to test the antitumor activity of the obtained compounds in vitro.Five new candidate compounds with the same skeleton were screened and their structures were confirmed by^(1)H-NMR and^(13)C-NMR.The results showed that the inhibitory effect of the tested compounds on A549 and SGC7901 tumor cells was higher than that of oleanolic acid,especially compound R_(4)had significant antitumor activity.
作者
邬月娇
孟艳秋
WU Yue-jiao;MENG Yan-qiu(Shenyang University of Chemical Technology,Shenyang 110142,China)
出处
《沈阳化工大学学报》
CAS
2022年第3期210-214,共5页
Journal of Shenyang University of Chemical Technology
基金
国家自然科学基金(21372156)
辽宁省创新团队资助立项(LT2017009)
辽宁省教育厅科研项目(LFD2017004)
辽宁省重点研发计划项目(2019JH2/10300034)
沈阳市重大科技成果转化项目(20-203-5-45)
辽宁省教育厅科学研究项目(LJ2020025)
沈阳化工大学重点攻关项目(LDB2019001)。
关键词
齐墩果酸类似物
结构修饰
抗肿瘤活性
oleanolic acid analogue
structural modification
antitumor activity
