Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
J Med Chem
; 48(16): 5092-5, 2005 Aug 11.
Article
em En
| MEDLINE
| ID: mdl-16078826
ABSTRACT
Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. Additional SAR, biological activity, and structural information from a tanaproget/hPR-LBD (hPR-LBD = human progesterone receptor ligand binding domain) cocrystal structure will also be presented.
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Oxazinas
/
Pirróis
/
Tionas
/
Receptores de Progesterona
/
Benzoxazinas
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article