Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series.
Steroids
; 138: 91-101, 2018 10.
Article
em En
| MEDLINE
| ID: mdl-29997047
ABSTRACT
Novel benzylidenes (chalcones) of the 16-dehydroprogesterone series have been characterized and their antitumor activity against two breast cancer cell lines was evaluated. Benzylidenes exhibit significant antiproliferative effect on cells and inhibit cell growth in hormone-dependent MCF-7 and hormone-independent MDA-MB-231 breast cancer cell lines. Compound 3d exhibits the highest activity against two breast cancer cell lines, with the IC50 value of about 2⯵M. Compounds 3e,m,n display considerable selectivity for hormone-dependent breast cancer cells, with the IC50 value lower than 6⯵M. Moreover, these steroidal benzylidenes regulate ERα signaling and reveal p53-independent mechanism of pro-apoptotic action in MCF-7 cells. The new class of antitumor compounds holds promise as the basis for the design of agents for cancer therapy.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
Progesterona
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Proliferação de Células
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Antineoplásicos
Limite:
Female
/
Humans
Idioma:
En
Revista:
Steroids
Ano de publicação:
2018
Tipo de documento:
Article