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Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2007 Sep 15; Vol. 15 (18), pp. 6170-81. Date of Electronic Publication: 2007 Jun 20. - Publication Year :
- 2007
-
Abstract
- A series of beta-sulfonyl hydroxamate TACE inhibitors, bearing a butynylamino or a butynyloxy P1' group, was designed and synthesized. Of the compounds investigated, 22 has excellent potency against isolated TACE enzyme, shows good selectivity over MMP-2 and MMP-13, and oral activity in an in vivo mouse model of TNF-alpha production.
- Subjects :
- ADAM Proteins metabolism
ADAM17 Protein
Animals
Matrix Metalloproteinase Inhibitors
Matrix Metalloproteinases metabolism
Mice
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Tumor Necrosis Factor-alpha metabolism
ADAM Proteins antagonists & inhibitors
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Hydroxamic Acids chemistry
Hydroxamic Acids pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0968-0896
- Volume :
- 15
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 17606376
- Full Text :
- https://doi.org/10.1016/j.bmc.2007.06.031