[Design, synthesis and activity evaluation of novel matrix metalloproteinases inhibitors based on the structure of enzyme].
Yao Xue Xue Bao
; 42(12): 1271-81, 2007 Dec.
Article
in Zh
| MEDLINE
| ID: mdl-18338640
ABSTRACT
A novel inhibitor series for matrix metalloproteinases (MMPs) were designed and synthesized. Using succinate and malonate as zinc binding groups and long hydrophobic substituents to bind with S1' pockets, the compounds showed micromolar inhibition and selectivity for MMP-2 over others. And we found a better activity compound. It is a chance to find a better precursor of MMP-2 inhibitors with activity and bioavailability by further optimization of compounds.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Drug Design
/
Matrix Metalloproteinases
/
Enzyme Inhibitors
/
Matrix Metalloproteinase Inhibitors
Language:
Zh
Journal:
Yao Xue Xue Bao
Year:
2007
Document type:
Article
Affiliation country:
China