1.
Bioorg Med Chem Lett
; 14(16): 4147-51, 2004 Aug 16.
Article
in English
| MEDLINE
| ID: mdl-15261259
ABSTRACT
A series of benzodiazepine MMP/TACE inhibitors bearing polar moieties has been synthesized in an effort to optimize inhibitory activity against LPS-stimulated TNF production in human monocytes and oral activity in a murine LPS model.
Subject(s)
Benzodiazepines/pharmacology , Enzyme Inhibitors/pharmacology , Matrix Metalloproteinase Inhibitors , Metalloendopeptidases/antagonists & inhibitors , ADAM Proteins , ADAM17 Protein , Animals , Cell Line , Enzyme Inhibitors/pharmacokinetics , Humans , Lipopolysaccharides/pharmacology , Mice , Mice, Inbred BALB C , Monocytes/drug effects , Monocytes/metabolism , Mouth/drug effects , Tumor Necrosis Factor-alpha/antagonists & inhibitors , Tumor Necrosis Factor-alpha/biosynthesis
2.
Bioorg Med Chem Lett
; 12(20): 2867-70, 2002 Oct 21.
Article
in English
| MEDLINE
| ID: mdl-12270165
ABSTRACT
A series of benzodiazepine inhibitors of the MMPs and TACE has been developed. These compounds display an interesting selectivity profile and should be useful tools for exploring the biological relevance of such selectivity.