期刊
CHEMMEDCHEM
卷 4, 期 3, 页码 352-362出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.200800324
关键词
inhibitors; matrix metalloproteinases; molecular modeling; phosphonic acids; zinc binding groups
资金
- Ministero dell'Istruzione, dell'Universita e della Ricerca (MIUR [2004031241_005]
Eleven simple alpha-sulfonylphosphonates, new analogues of previously reported alpha-sulfonylaminophosphonates, were prepared and tested as MMP inhibitors. The IC50 values of most of these compounds are in the nanomolar range against MMP-2, -8, -13, and -14. Compound 11 proved to be the most effective inhibitor of MMP-2 (IC50=60 nM), with interesting selectivity versus the anti-target enzymes MMP-3 and MMP-9. The mode of binding of the new phosphonates in the active site of MMP-2 was studied, and variations in inhibition was explained by means of molecular modeling.
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