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1.
Bioorg Med Chem ; 19(10): 3060-73, 2011 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-21530273

RESUMO

The synthesis of some natural and synthetic biflavonoids was performed in good overall yields starting from readily available materials via high yielding aldol and Ullmann condensations. Some of these compounds, especially bichalcones, display an interesting activity against fungi, higher than that of the corresponding monomers.


Assuntos
Antifúngicos/síntese química , Antifúngicos/farmacologia , Biflavonoides/síntese química , Biflavonoides/farmacologia , Fungos/efeitos dos fármacos , Antifúngicos/química , Biflavonoides/química , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Micoses/tratamento farmacológico
2.
Bioorg Med Chem ; 15(10): 3356-67, 2007 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-17383189

RESUMO

A series of synthetic chalcones, flavanones, and flavones has been synthesized and evaluated for antitumor activity against the human kidney carcinoma cells TK-10, human mammary adenocarcinoma cells MCF-7 (estrogen receptor-positive), and human colon adenocarcinoma cells HT-29. The most active series is the chalcone ones with the best results against TK-10 and HT-29 cells. Fourteen out of 53 analyzed compounds resulted very active against at least two of the studied tumoral cells. Alkaline single cell gel electrophoresis, comet assay, was performed as a study of the chromosomal aberrations promoted by the compounds on normal cells. Four active and two inactive chalcones were studied in the comet assay against normal human kidney cells (HK-2). A structure-activity relationship analysis of these compounds was performed and for 4- and 3,4-disubstituted derivatives a quantitative correlation was obtained in the case of anti-HT-29 activity.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Chalconas/síntese química , Chalconas/farmacologia , Flavonas/síntese química , Flavonas/farmacologia , Linhagem Celular Tumoral , Cromatografia em Camada Fina , Aberrações Cromossômicas/efeitos dos fármacos , Ensaio Cometa , Dano ao DNA , DNA de Neoplasias/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Espectrofotometria Infravermelho , Relação Estrutura-Atividade , Difração de Raios X
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