New 3ß-hydroxysteroid-indolamine conjugates: Design, synthesis and inhibition of C6 glioma cell proliferation.
Steroids
; 164: 108728, 2020 12.
Article
em En
| MEDLINE
| ID: mdl-32931809
ABSTRACT
Four novel indole steroids based on dehydroepiandrosterone (IS-1), estrone (IS-2) and pregnenolone (IS-3) were obtained and studied for their ability to inhibit C6 glioma proliferation. A reduction in cell proliferation by 52 ± 13% was observed for IS-1 at 10 µM, whereas IS-3 and abiraterone acetate at 10 µM caused a 36 ± 8% decrease. Surprisingly, the cellular effects reported for abiraterone, namely, cytochrome P450 CYP17A1 inhibition and endoplasmic reticulum stress were not detected for IS-1. However, both abiraterone and IS-1 significantly increased glutathione levels. Docking studies predicted good affinity of IS-1 to liver X receptors and regulatory protein Keap1, which are proposed to be involved in the compounds' antiproliferative activity.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias Encefálicas
/
Desenho de Fármacos
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Proliferação de Células
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Glioma
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Hidroxiesteroides
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Indóis
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Revista:
Steroids
Ano de publicação:
2020
Tipo de documento:
Article