Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.
J Med Chem
; 52(5): 1247-50, 2009 Mar 12.
Article
em En
| MEDLINE
| ID: mdl-19215087
ABSTRACT
A three-dimensional pharmacophore model was generated utilizing a set of known inhibitors of c-Myc-Max heterodimer formation. The model successfully identified a set of structurally diverse compounds with potential inhibitory activity against c-Myc. Nine compounds were tested in vitro, and four displayed affinities in the micromolar range and growth inhibitory activity against c-Myc-overexpressing cells. These studies demonstrate the applicability of pharmacophore modeling to the identification of novel and potentially more puissant inhibitors of the c-Myc oncoprotein.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Modelos Moleculares
/
Proteínas Proto-Oncogênicas c-myc
/
Fatores de Transcrição de Zíper de Leucina e Hélice-Alça-Hélix Básicos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Estados Unidos