Novel 4-phenoxypyridine derivatives bearing imidazole-4-carboxamide and 1,2,4-triazole-3-carboxamide moieties: Design, synthesis and biological evaluation as potent antitumor agents.
Bioorg Chem
; 120: 105629, 2022 03.
Article
en En
| MEDLINE
| ID: mdl-35078047
ABSTRACT
Two series of novel 4-phenoxypyridine derivatives containing imidazole-4-carboxamide and 4-methyl-5-oxo-4,5-dihydro-1,2,4-triazole-3-carboxamide moieties were synthesized and evaluated for their in vitro inhibitory activities against c-Met kinase and antiproliferative activities against MKN-45, A549 and H460 cancer cell lines. The results indicated that most of the compounds showed moderate to good antitumor activities. The most promising compound T14 (with c-Met IC50 value of 0.012 µM) showed remarkable antiproliferative activities against MKN-45, A549 and H460 cell lines with IC50 values of 0.64 µM, 1.92 µM and 2.68 µM, respectively. Their preliminary structure-activity relationships (SARs) studies indicate that imidazole-4-carboxamide was more preferred as linker part, and electron-withdrawing groups (especially halogen groups) on the terminal phenyl rings were beneficial for improving the antitumor activities.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Quinolinas
/
Antineoplásicos
Tipo de estudio:
Prognostic_studies
Idioma:
En
Año:
2022
Tipo del documento:
Article