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Chem Biol Drug Des ; 84(1): 86-91, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24476543

RESUMO

Derivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects of (i) the heterocyclic ring, (ii) the alkoxy group at position 5 of the benzoxathiole ring, and (iii) the substituents in the phenyl ring B. Replacement of the sulfur atom by oxygen does not influence the activity. None of the listed structural fragments alone assured high cytotoxic activity.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Derivados de Benzeno/química , Derivados de Benzeno/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Compostos de Sulfidrila/química , Compostos de Sulfidrila/farmacologia , Linhagem Celular Tumoral , Chalconas/química , Chalconas/farmacologia , Humanos , Neoplasias/tratamento farmacológico , Relação Estrutura-Atividade
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