Design, Synthesis, and Anti-Breast Cancer Activity of Novel Fluorinated 7-O-Modified Genistein Derivatives.
Med Chem
; 19(1): 64-74, 2022.
Article
em En
| MEDLINE
| ID: mdl-35674304
ABSTRACT
BACKGROUND:
Genistein has been limited in clinical application due to its low bioavailability, extremely poor liposolubility, and fast glycosylation rate, though it possesses anti-breast cancer activity. Therefore, the discovery of novel genistein derivatives is an urgency.OBJECTIVE:
To enhance the anti-breast cancer activity of genistein, a series of novel fluorinated genistein derivatives were synthesized.METHODS:
Their in vitro antitumor activity was investigated by the MTT assay against three cancer cell lines, via, MDA-MB-231, MCF-7, and MDA-MB-435, respectively.RESULTS:
Analogs 1d, 2b, and 3b showed remarkable anticancer activities compared to tamoxifen, a clinical anti-breast cancer drug on the market.CONCLUSION:
The activities against breast cancer of genistein were enhanced by introducing the 7- alkoxyl group and fluorine atom into the B-ring. Therefore, these compounds may be potential candidates for treating breast cancer.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Mama
/
Antineoplásicos
Limite:
Female
/
Humans
Idioma:
En
Revista:
Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2022
Tipo de documento:
Article