Synthesis and activity evaluation of allyl-quercetin derivatives / 中国药学杂志
Chinese Pharmaceutical Journal
;
(24): 442-448, 2016.
Artículo
en Chino
| WPRIM
| ID: wpr-859168
ABSTRACT
OBJECTIVE:
To design and synthesize two kinds of allyl-substituted quercetin and investigate their anti-oxidation and anti-tumor activities in vitro.METHODS:
The target compounds 1 and 2 were first synthesized from quercetin by hydroxyl protection, allylation,Claisen rearrangement and deprotection. The anti-oxidation and anti-tumor activities of the target compounds and intermediate products were evaluated by DPPH and MTT assay.RESULTS:
Eight compounds were synthesized,including six intermediates and two target compounds,in which four were new compounds. All of them were confirmed by 1H-NMR,13C-NMR and LC-MS spectra. The anti-oxidation and anti-tumor tests showed that compounds 1,2,5,6,8 and 9 had anti-oxidation activities and compound 5 inhibited A549 lung cancer cell proliferation. Compound 9 could inhibit the proliferation of lung cancer A549 cells and HepG2 cells.CONCLUSION:
The compounds with electron-donating groups have significant anti-oxidant activity. When acetyl and methyl ether groups are used as the protecting groups,the position of introducing allyl group to quercetin has obvious impact on the anti-tumor activity.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Idioma:
Chino
Revista:
Chinese Pharmaceutical Journal
Año:
2016
Tipo del documento:
Artículo
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