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Chem Biodivers ; 10(11): 1999-2006, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24243608

RESUMO

A series of chalcone derivatives, 1-15, were prepared by Claisen-Schmidt condensation and evaluated for their cytotoxicities on tumor cell lines and also against proteolytic enzymes such as cathepsins B and K. Of the compounds synthesized, (E)-3-(3,4-dimethoxyphenyl)-1-phenylprop-2-en-1-one (12), (E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one (13), (E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one (14), and (E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one (15) showed significant cytotoxicities. The most effective compound was 15, which showed high cytotoxic activity with an IC50 value lower than 1 µg/ml, and no selectivity on the tumor cells evaluated. Substituents at C(4) of ring B were found to be essential for cytotoxicity. In addition, it was also demonstrated that some of these chalcones are moderate inhibitors of cathepsin K and have no activity against cathepsin B.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Catepsina B/antagonistas & inibidores , Catepsina K/antagonistas & inibidores , Chalcona/análogos & derivados , Chalcona/farmacologia , Catepsina B/metabolismo , Catepsina K/metabolismo , Linhagem Celular Tumoral , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/enzimologia
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