Design, synthesis and biological evaluation of novel 3-(2-oxo-2-substituted acetamido)benzamides as PARP-1 inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 738-745, 2015.
Artigo
em Chinês
| WPRIM
| ID: wpr-257074
ABSTRACT
Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Benzamidas
/
Desenho de Fármacos
/
Química
/
Poli(ADP-Ribose) Polimerases
/
Reparo do DNA
/
Simulação de Acoplamento Molecular
/
Inibidores de Poli(ADP-Ribose) Polimerases
/
Antineoplásicos
Tipo de estudo:
Estudo prognóstico
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2015
Tipo de documento:
Artigo
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