Cytotoxic Activity and Quantitative Structure Activity Relationships of Arylpropyl Sulfonamides
The Korean Journal of Physiology and Pharmacology
;
: 237-243, 2013.
Artigo
em Inglês
| WPRIM
| ID: wpr-727724
ABSTRACT
B13 is a ceramide analogue and apoptosis inducer with potent cytotoxic activity. A series of arylpropyl sulfonamide analogues of B13 were evaluated for their cytotoxicity using MTT assays in prostate cancer PC-3 and leukemia HL-60 cell lines. Some compounds (4, 9, 13, 14, 15, and 20) showed stronger activities than B13 in both tumor cell lines, and compound (15) gave the most potent activity with IC50 values of 29.2 and 20.7 microM, for PC-3and HL-60 cells, respectively. Three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed to build highly reliable and predictive CoMSIA models with cross-validated q2 values of 0.816 and 0.702, respectively. Our results suggest that long alkyl chains and a 1R, 2R configuration of the propyl group are important for the cytotoxic activities of arylpropyl sulfonamides. Moreover, the introduction of small hydrophobic groups in the phenyl ring and sulfonamide group could increase biological activity.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Neoplasias da Próstata
/
Sulfonamidas
/
Leucemia
/
Apoptose
/
Células HL-60
/
Concentração Inibidora 50
/
Relação Quantitativa Estrutura-Atividade
/
Linhagem Celular Tumoral
Tipo de estudo:
Estudo prognóstico
Limite:
Humanos
Idioma:
Inglês
Revista:
The Korean Journal of Physiology and Pharmacology
Ano de publicação:
2013
Tipo de documento:
Artigo
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