Synthesis and structure guided evaluation of estrogen agonist and antagonist activities of some new tetrazolyl indole derivatives.
Eur J Med Chem
; 43(10): 2149-58, 2008 Oct.
Article
em En
| MEDLINE
| ID: mdl-18155810
ABSTRACT
Several regioisomeric tetrazolyl indole derivatives with structurally modified alkyl substituents at the tetracyclic indole nitrogen containing N-ethyl amino tetrazole moiety have been synthesized and screened for their ER binding affinity, agonist (estrogenic), antagonist (antiestrogenic) and anti-implantation activities. N-2 regioisomers were found to be moderately antagonists and one compound showed 100% contraceptive efficacy at 10 mg/kg dose. Molecular docking studies carried out in comparison to estradiol and raloxifene showed different binding modes of the two regioisomers to the binding site.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tetrazóis
/
Antagonistas de Estrogênios
/
Estrogênios
/
Indóis
Limite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Índia