Design, synthesis and activities of novel benzothiazole derivatives containing arylpiperazine / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1259-1265, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-259485
ABSTRACT
Twenty-four novel benzothiazole derivatives containing arylpiperazine were designed and synthesized by bioisosterism principle. Anti-proliferative effect of these synthesized compounds against four cancer cell and two normal cell lines were evaluated in vitro by the standard MTT assay. Pharmacological test showed that most of the compounds exhibited potent antitumor activity. Some of the compounds (II2, II3, II6, II7) showed strong anti-proliferation activities against HepG2 and HeLa229 cell lines with the IC 50 values of 1.6-4.5 micromol x L(-1) and 2.5-5.3 micromol x L(-1), respectively, and compounds having cyan in p-substituted benzene ring (I4, I8, I12, II4, II8 and II12) were found to have better antitumor activities against AsPC-1 cell lines with the IC50 values of 5.2-11.3 micromol x L(-1). The structure-activity relationship of benzothiazole derivatives containing arylpiperazine was also discussed preliminarily.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Piperazinas
/
Relação Estrutura-Atividade
/
Ensaios de Seleção de Medicamentos Antitumorais
/
Estrutura Molecular
/
Química
/
Concentração Inibidora 50
/
Linhagem Celular Tumoral
/
Proliferação de Células
/
Benzotiazóis
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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