Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.
Bioorg Med Chem Lett
; 30(23): 127610, 2020 12 01.
Article
em En
| MEDLINE
| ID: mdl-33045329
ABSTRACT
In this work three novel series of c-Met/HDAC bifunctional inhibitors were designed and synthesized by merging pharmacophores of c-Met and HDAC inhibitors. The most potent compound 11j inhibited c-Met kinase and HDAC1 with IC50 values of 21.44 and 45.22 nM, respectively. In addition, 11j showed efficient antiproliferative activities against both MCF-7 and A549 cells with greater potency than the reference drug SAHA and Cabozantinib. This work may lay the foundation for developing novel dual c-Met/HDAC inhibitors as potential anticancer therapeutics.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteínas Proto-Oncogênicas c-met
/
Inibidores de Proteínas Quinases
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Histona Desacetilase 1
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Inibidores de Histona Desacetilases
/
Antineoplásicos
Tipo de estudo:
Prognostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article