1.
Bioorg Med Chem Lett
; 11(16): 2147-51, 2001 Aug 20.
Article
in English
| MEDLINE
| ID: mdl-11514157
ABSTRACT
N-Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-alpha converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmacokinetics in the rat and dog.
Subject(s)
Enzyme Inhibitors/pharmacology , Formamides/pharmacology , Matrix Metalloproteinase Inhibitors , Metalloendopeptidases/antagonists & inhibitors , Oligopeptides/pharmacology , ADAM Proteins , ADAM17 Protein , Animals , Dogs , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacokinetics , Formamides/chemistry , Oligopeptides/chemistry , Rats , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 11(14): 1939-42, 2001 Jul 23.
Article
in English
| MEDLINE
| ID: mdl-11459665
ABSTRACT
We have prepared a novel series of 2-amino-4,6-diarylpyridines that function as ligands of estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). These compounds bind to both ERalpha and ERbeta with a modest selectivity for the alpha subtype. The most potent of these analogues, compound 19, has a K(i)=20nM at ERalpha. These molecules represent a novel template for designing potentially useful ligands for the estrogen receptor.
Subject(s)
Receptors, Estrogen/metabolism , Selective Estrogen Receptor Modulators/chemical synthesis , Selective Estrogen Receptor Modulators/pharmacology , Bacteria/genetics , Bacteria/metabolism , Binding Sites/physiology , Crystallography, X-Ray , Estrogen Receptor alpha , Estrogen Receptor beta , Humans , Ligands , Protein Binding/physiology , Pyridines/chemical synthesis , Pyridines/metabolism , Raloxifene Hydrochloride/metabolism , Sensitivity and Specificity
3.
J Med Chem
; 39(3): 665-8, 1996 Feb 02.
Article
in English
| MEDLINE
| ID: mdl-8576907
