Synthesis and preliminary anti-tumor activity of novel ursolic acid derivative-chalcone conjugates / 中国药科大学学报
Journal of China Pharmaceutical University
; (6): 31-41, 2017.
Article
en Zh
| WPRIM
| ID: wpr-514221
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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.
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Zh
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Journal of China Pharmaceutical University
Año:
2017
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Article