Synthesis and preliminary anti-tumor activity of novel ursolic acid derivative-chalcone conjugates
10.11665/j.issn.1000-5048.20170105
- VernacularTitle:新型熊果酸衍生物与查耳酮缀合物的合成及其抗肿瘤活性初步评价
- Author:
Ting PEI
;
Yuying WANG
- Keywords:
ursolic acid derivative-chalcone conjugates;
synthesis;
anti-tumor activity
- From:
Journal of China Pharmaceutical University
2017;48(1):31-41
- CountryChina
- Language:Chinese
-
Abstract:
Ten novel conjugates with ursolic acid core and different chalcone ligands were synthesized via esteri-fication using the natural ursolic acid as starting material. The structures of these conjugates were confirmed by 1 H NMR, 13 C NMR and HRMS. The preliminary biological results showed that these compounds displayed signifi-cant antiproliferative effect on CNE2, KB, MCF-7, A549 and HepG2 cells. These compounds were more effective than ursolic acid and tamoxifen against MCF-7 cells. Especifically, compound 11e ( IC50 =4. 7 μmol/L) showed the greatest potency against MCF-7, which was about 3-times more potent than tamosifen ( IC50 =15. 2 μmol/L) . Additionally, all conjugates were nontoxic to health MCF-10A and VERO cells, and had higher security than tamoxifen.
