Structure-activity relationship of halophenols as a new class of protein tyrosine kinase inhibitors.
Int J Mol Sci
; 12(9): 6104-15, 2011.
Article
em En
| MEDLINE
| ID: mdl-22016647
A series of new benzophenone and diphenylmethane halophenol derivatives were prepared. Their structures were established based on (1)H NMR, (13)C NMR and HRMS data. All prepared compounds were screened for their in vitro protein tyrosine kinase (PTK) inhibitory activities. The effects of modification of the linker, functional groups and substituted positions at the phenyl ring on PTK inhibitory activity were investigated. Twelve halophenols showed significant PTK inhibitory activity. Among them, compounds 6c, 6d, 7d, 9d, 10d, 11d and 13d exhibited stronger activities than that of genistein, the positive reference compound. The results gave a relatively full and definite description of the structure-activity relationship and provided a foundation for further design and structure optimization of the halophenols.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Fenóis
/
Proteínas Tirosina Quinases
/
Inibidores de Proteínas Quinases
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Halogênios
Limite:
Animals
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article