Synthesis and antitumor activity of novel tetrahydro-beta-carboline derivatives as KSP inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1119-1123, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-259506
ABSTRACT
Inhibitors of kinesin spindle protein (KSP) are a promising class of anticancer agents that cause mitotic arrest and induce apoptosis of tumor cells. A series of novel tetrahydro-beta-carboline derivatives were synthesized as kinesin spindle protein inhibitor and evaluated as potential antitumor agents. All compounds showed promising KSP inhibitiory activity. Compounds 8 and 9 exhibited better antitumor activity (Lung/A549, Stomach/AGS) than CK0106023 with GI50/IC50 values (1.07/1.62 and 1.46/3.27 micromol x L(-1), 1.09/>10 and 1.22/6.33 micromol x L(-1), respectively).
Texto completo:
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Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Carbolinas
/
Estrutura Molecular
/
Química
/
Cinesinas
/
Concentração Inibidora 50
/
Linhagem Celular Tumoral
/
Proliferação de Células
/
Antineoplásicos
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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