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Daru ; 23: 36, 2015 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-26197788

RESUMO

BACKGROUND: Recent studies have been explained the role of lipoxygenases (LOX) in the origin of cancer. Among the lipoxygenases, the 5-LOX, 12-LOX and 15-LOX are more important in the cause of neoplastic disorders. In the present investigation, a new series of anticancer agents with 1,3,4-thiadiazole and phthalimide substructures were synthesized and their in vitro cytotoxicity was evaluated by MTT assay. Moreover, enzyme inhibitory potency was also assessed by enzymatic protocol towards 15-LOX-1. Molecular docking was performed to explore in silico binding mode of the target compounds. RESULTS: Tested compounds showed a better cytotoxic activity against HT29 cell line (colorectal cancer) in comparison with other cell lines (PC3: prostate carcinoma; SKNMC: neuroblastoma). Unfortunately, all of the tested derivatives rendered lower inhibitory potency than quercetin towards 15-LOX-1. Four hydrogen bonds were detected in docking studies for compound 4d as the most potent derivative in enzymatic assay. CONCLUSIONS: The biological results of reported compounds in this research were not so satisfactory. But, further structural modifications are necessary to improve the bioactivity of these derivatives.


Assuntos
Araquidonato 15-Lipoxigenase/metabolismo , Inibidores de Lipoxigenase/farmacologia , Ftalimidas/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Inibidores de Lipoxigenase/síntese química , Modelos Moleculares , Simulação de Acoplamento Molecular , Ftalimidas/síntese química , Relação Estrutura-Atividade
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