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1.
Biosci Biotechnol Biochem ; 77(9): 1981-3, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24018685

RESUMO

Tea catechins have strong bitterness and influence the taste of tea. Among the 25 human bitter-taste receptors (TAS2Rs), we found that hTAS2R14 responded to catechins, in addition to hTAS2R39, a known catechin receptor. Although hTAS2R14 responded to (-)-epicatechin gallate and (-)-epigallocatechin gallate, it did not respond to (-)-epicatechin and (-)-epigallocatechin.


Assuntos
Catequina/análogos & derivados , Receptores Acoplados a Proteínas G/metabolismo , Cálcio/metabolismo , Catequina/farmacologia , Relação Dose-Resposta a Droga , Células HEK293 , Humanos
2.
Chem Pharm Bull (Tokyo) ; 53(2): 153-63, 2005 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-15684512

RESUMO

A series of novel 3-[4-phenyl-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes and related compounds were synthesized and evaluated by their cytotoxic activity against several tumor cell lines in vitro and in vivo antitumor activity against some tumor models when administered both intraperitoneally and orally. Compounds with the 3-chloropyridin-2-yl group (9g) and the 3-fluoro-5-substituted phenylpiperazinyl group (29b, c, and e) showed significantly potent cytotoxicity by in vitro testing. Among them, the 3-cyano-5-fluorophenyl derivative (29b) exhibited potent antitumor activity against several tumor cells including human carcinoma without causing undesirable effects in mice.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Piperazinas/síntese química , Piperazinas/farmacologia , Propano/análogos & derivados , Propano/síntese química , Propano/farmacologia , Animais , Linhagem Celular Tumoral , Fenômenos Químicos , Físico-Química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Transplante de Neoplasias , Relação Estrutura-Atividade
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