| Literature DB >> 10411481 |
S Vassiliou1, A Mucha, P Cuniasse, D Georgiadis, K Lucet-Levannier, F Beau, R Kannan, G Murphy, V Knäuper, M C Rio, P Basset, A Yiotakis, V Dive.
Abstract
Several phosphinic pseudo-tripeptides of general formula R-XaaPsi(PO(2)-CH(2))Xaa'-Yaa'-NH(2) were synthesized and evaluated for their in vitro activities to inhibit stromelysin-3, gelatinases A and B, membrane type-1 matrix metalloproteinase, collagenases 1 and 2, and matrilysin. With the exception of collagenase-1 and matrilysin, phosphinic pseudo-tripeptides behave as highly potent inhibitors of matrix metalloproteinases, provided they contain in P(1)' position an unusual long aryl-alkyl substituent. Study of structure-activity relationships regarding the influence of the R and Xaa' substituents in this series may contribute to the design of inhibitors able to block only a few members of the matrix metalloproteinase family.Entities:
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Year: 1999 PMID： 10411481 DOI： 10.1021/jm9900164
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446