RESUMO
A series of valproic acid salicylanilide esters were designed and synthesized based on the principle of prodrug. The structures of the target compounds were confirmed by MS, 1H NMR and 13C NMR. Anti-tumor activities of these compounds against K562, A549, A431 cells in vitro were investigated by MTT assay and SRB assay. The results indicated that the compounds 6h-6j were found to have stronger cell growth inhibitory action than gefitinib, and comparable to niclosamide, which are worth to be intensively studied further.
Assuntos
Humanos , Antineoplásicos , Química , Farmacologia , Linhagem Celular Tumoral , Proliferação de Células , Desenho de Fármacos , Ésteres , Concentração Inibidora 50 , Células K562 , Estrutura Molecular , Pró-Fármacos , Química , Farmacologia , Salicilanilidas , Química , Farmacologia , Relação Estrutura-Atividade , Ácido Valproico , Química , FarmacologiaRESUMO
Ferulic acid, an useful compound of Chinese traditional medicine, was used as leading compound. Six ferulic acid derivatives were designed and synthesized based on bioisosterism. Their structures were characterized by IR, 1H NMR, 13C NMR and mass spectra. In vivo experiment showed that ferulic acid derivatives had good inhibitory effects on adenosine diphosphate (ADP) induced platelet aggregation, which were significantly higher than that of Ozagrel.