Synthesis and anti-tumor activity of ursolic acid-triazole derivatives
10.16438/j.0513-4870.2024-0698
- VernacularTitle:熊果酸-三氮唑衍生物的合成及抗肿瘤活性研究
- Author:
Zhen-yu KUAI
1
;
Yan-qiu MENG
2
Author Information
1. Department of Pharmacy Teaching and Research, Maanshan Technical College, Maanshan
2. Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang
- Publication Type:Research Article
- Keywords:
ursolic acid;
molecular docking;
c-Kit;
structural modification;
anti-tumor activity
- From:
Acta Pharmaceutica Sinica
2025;60(1):172-178
- CountryChina
- Language:Chinese
-
Abstract:
Ten ursolic acid derivatives were designed from the lead compound ursolic acid by introducing 1,2,3-triazole at C-3 and C-28. The target compounds were synthesized and characterized by 1H NMR and 13C NMR. MTT assay was used to study the antitumor activity of these compounds in human cancer cells with high expression (MCF-7 and SGC-7901). The results showed that the antitumor activity of all compounds on MCF-7 and SGC-7901 tumor cells was significantly higher than that of ursolic acid. The compound II4 exhibited significant antitumor activity which was equivalent to the positive control drug nilotinib, molecular docking showed that the compound II4 have high binding ability with c-Kit, which deserves further research.
