Synthesis and Smo Activity of Some Novel Benzamide Derivatives.
Molecules
; 23(1)2017 Dec 31.
Article
em En
| MEDLINE
| ID: mdl-29301237
ABSTRACT
Two series of benzamides compounds bearing piperidine groups were synthesized and the Gli-luc luciferase activity was screened by Gys-luc luciferase gene detection method. Compound 5q showed promising inhibition of hedgehog (Hh) signaling pathway. To further verify whether the Hh inhibitory activities of the target compounds are derived from their inhibition to the Smoothened (Smo) receptor, the compounds with good potency were evaluated in a fluorescence competitive displacement assays, the results showed the Smo inhibitory potency of these compounds correlated well with their Hh inhibition, which suggested that the observed Hh activity was driven by Smo inhibitors.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Benzamidas
/
Receptor Smoothened
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article