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

RESUMEN

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.


Asunto(s)
Amidas/química , Antiinflamatorios no Esteroideos/síntesis química , Pirazoles/química , Amidas/síntesis química , Amidas/uso terapéutico , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/uso terapéutico , Carragenina/toxicidad , Edema/inducido químicamente , Edema/tratamiento farmacológico , Ratas
2.
Eur J Med Chem ; 45(11): 4720-5, 2010 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-20817327

RESUMEN

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.


Asunto(s)
Ácidos Carboxílicos/química , Pirazoles/síntesis química , Pirazoles/farmacología , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Resonancia Magnética , Pirazoles/química , Espectrometría de Masa por Ionización de Electrospray , Espectroscopía Infrarroja por Transformada de Fourier
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