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Synthesis, characterization and in vitro anti-proliferative effects of pentacyclic triterpenoids
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-09-17 , DOI: 10.1007/s00044-021-02795-6
Qian Wang 1 , Yandan Liu 1 , Lei Sun 1 , Bo Lu 1 , Longxuan Zhao 1, 2 , Mei Jin 3 , Gao Li 3
Affiliation  

A series of glycyrrhetinic acid, oleanolic acid and ursolic acid derivatives were designed and synthesized. Structures of all novel compounds were determined by 1H NMR, 13C NMR, and HRMS methods. In vitro anti-proliferative effects of all compounds were evaluated against A549, Hela and HepG2 cancer cell lines. The three compounds G2, G3 and G4 showed better anti-proliferative effects than the positive control doxorubicin on the three kinds of cancer cells. The two compounds O1 and U11 showed better anti-proliferative effects than doxorubicin on Hela cells. The four compounds O2, O3, O8 and U8 showed better anti-proliferative effects than doxorubicin on HepG2 cells. Notably, compound G3 demonstrated the strongest growth inhibitory effects with IC50 values of 0.16 ± 0.23 µM and 0.33 ± 0.41 µM on Hela and HepG2 cells, respectively, and compound G2 demonstrated the strongest growth inhibitory effect with IC50 values of 0.80 ± 1.03 µM on A549 cells.



中文翻译:

五环三萜类化合物的合成、表征和体外抗增殖作用

设计合成了一系列甘草次酸、齐墩果酸和熊果酸衍生物。所有新化合物的结构均通过1 H NMR、13 C NMR 和 HRMS 方法确定。评估了所有化合物对 A549、Hela 和 HepG2 癌细胞系的体外抗增殖作用。三种化合物G2G3G4对三种癌细胞显示出比阳性对照阿霉素更好的抗增殖作用。两种化合物O1U11对Hela细胞显示出比阿霉素更好的抗增殖作用。四种化合物O2 , O3 , O8U8表现出比对HepG2细胞阿霉素更好的抗增殖作用。值得注意的是,化合物G3对 Hela 和 HepG2 细胞的生长抑制作用最强,IC 50值分别为 0.16 ± 0.23 µM 和 0.33 ± 0.41 µM,化合物G2的生长抑制作用最强,IC 50值为 0.80 ± 1.03 µM在 A549 细胞上。

更新日期:2021-09-17
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