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1.
Bioorg Med Chem Lett ; 21(14): 4138-40, 2011 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-21689936

RESUMO

A new series of 3-phenyl-N-[3-(4-phenylpiperazin-1yl)propyl]-1H-pyrazole-5-carboxamide derivatives were synthesized and investigated their anti-inflammatory activities using carrageenan-induced rat paw edema model in vivo. All the synthesized compounds were found to be potent anti-inflammatory agents.


Assuntos
Amidas/química , Anti-Inflamatórios não Esteroides/síntese química , Pirazóis/química , Amidas/síntese química , Amidas/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/uso terapêutico , Carragenina/toxicidade , Edema/induzido quimicamente , Edema/tratamento farmacológico , Ratos
2.
Eur J Med Chem ; 45(11): 4720-5, 2010 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-20817327

RESUMO

Several novel molecules, 1-(3'-(9H-carbazol-4-yloxy)-2'-hydroxypropyl)-3-aryl-1H-pyrazole-5-carboxylic acid derivatives 3a-g were synthesized and screened to evaluate their cytotoxicity against cancer cells in vitro. The compounds 3a-g has been prepared by the reaction of ethyl 3-aryl-1H-pyrazole-5-carboxylate with 4-oxiranylmethoxy-9H-carbazole in moderate to excellent yields. The cytotoxicity of synthesized compounds was evaluated by a SRB (sulforhodamine B) assay against cancer cell such as SK-N-SH human neuroblastoma (NB), human A549 lung carcinoma, human breast cancer MCF-7 cell lines. The results showed that seven compounds can suppress SK-N-SH tumor cancer cell growth. Among them, compound 3d was the most effective small molecule in inhibiting SK-N-SH cell growth.


Assuntos
Ácidos Carboxílicos/química , Pirazóis/síntese química , Pirazóis/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Pirazóis/química , Espectrometria de Massas por Ionização por Electrospray , Espectroscopia de Infravermelho com Transformada de Fourier
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