Design, synthesis and antitumor activity of phthalazine-1,4-dione-based menaquinone analogs.
Bioorg Med Chem Lett
; 43: 128065, 2021 07 01.
Article
em En
| MEDLINE
| ID: mdl-33915257
ABSTRACT
New chemotherapeutics are needed to treat hepatocellular carcinoma (HCC), and menaquinones, homologs of vitamin K consisting of a 1,4-naphthoquinone core and a (poly)isoprene chain, are potential candidates. In this study, we designed and synthesized a series of phthalazine-1,4-dione-based menaquinone analogs. Among them, compounds bearing the intact isoprene chain exhibited selective antiproliferative activity towards HCC cell line JHH7, as compared with normal hepatocytes. The geranyl derivative 10 showed submicromolar potency, and might be a promising lead compound for anticancer agents.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Ftalazinas
/
Desenho de Fármacos
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Vitamina K 2
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Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Japão