Design, synthesis and biological evaluation of novel 7H-benzo [c] [1, 3] dioxolo [4, 5-f] chromen-7-one derivatives with potential anti-tumor activity.
Bioorg Chem
; 105: 104381, 2020 12.
Article
em En
| MEDLINE
| ID: mdl-33113412
ABSTRACT
In this study, a series of novel 7H-benzo [c] [1,3] dioxolo [4, 5-f] chromen-7-one derivatives were obtained by structural modification of the lead compounds with Fissitungfine B. A total 15 compounds were designed, synthesized and evaluated as inhibitors of tumor. These target compounds have the novel chemical structures that named three six-membered rings including one lactone six-membered ring. In vitro assay, the results showed that the target compounds have a broad spectrum and strong of anti-tumor activity. Such as the target compound 4n to MCF-7 was IC50 = 0.35 ± 0.01 µM, to A-549 was IC50 = 0.37 ± 0.01 µM, to Hela was IC50 = 0.56 ± 0.02 µM, to MDC-803 was IC50 = 0.53 ± 0.02 µM and COLO-205 was IC50 = 0.50 ± 0.02 µM in vitro. At the same time, in vivo anti-tumor activity assay results showed that the target compounds had a good inhibitory effect on tumor growth. Among them, the target compound 4n had the best anti-tumor activity, it could inhibit tumor growth well at a low dose. The target compound 4n could be used as a candidate drug for further research and development, in order to be used as early as application in the clinical treatment of tumors.
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Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
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Cromonas
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Antineoplásicos
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article