1.
Bioorg Med Chem
; 14(10): 3455-66, 2006 May 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16427291
RESUMO
The anti-inflammatory activity of non-selective estrogens has been attributed to their ability to antagonize the activity of nuclear factor kappaB (NF-kappaB), a known mediator of inflammatory responses. Here we report the identification of a potent new class of pathway-selective ER ligands that selectively antagonize NF-kappaB functional activity, while exhibiting a lack of classical estrogenic effect.
Assuntos
Quinoxalinas/síntese química , Receptores de Estrogênio/metabolismo , Células Cultivadas , Avaliação Pré-Clínica de Medicamentos , Humanos , Ligantes , Estrutura Molecular , NF-kappa B/antagonistas & inibidores , NF-kappa B/efeitos dos fármacos , Quinoxalinas/química , Quinoxalinas/farmacologia , Receptores de Estrogênio/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos
2.
Bioorg Med Chem Lett
; 16(4): 854-8, 2006 Feb 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16300947
RESUMO
The transcription factor nuclear factor-kappaB (NF-kappaB) is a key component in the onset of inflammation. We describe here a series of 4-hydroxyphenyl sulfonamide estrogen receptor (ER) ligands that selectively inhibit NK-kappaB transcriptional activity but are devoid of conventional estrogenic activity.