PHOSPHINIC ACID INHIBITORS OF MATRIX METALLOPROTEINASES

Authors
CALDWELL CG SAHOO SP POLO SA EVERSOLE RR LANZA TJ MILLS SG NIEDZWIECKI LM IZQUIERDOMARTIN M CHANG BC HARRISON RK KUO DW LIN TY STEIN RL DURETTE PL HAGMANN WK
Citation
Cg. Caldwell et al., PHOSPHINIC ACID INHIBITORS OF MATRIX METALLOPROTEINASES, Bioorganic & medicinal chemistry letters, 6(3), 1996, pp. 323-328
Citations number
25
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
3
Year of publication
1996
Pages
323 - 328
Database
ISI
SICI code
0960-894X(1996)6:3<323:PAIOMM>2.0.ZU;2-A
Abstract
The matrix metalloproteinase stromelysin-1 (MMP-3) is inhibited more s trongly by peptidyl phosphinic acid 7 than by its corresponding phosph onamidate and phosphonate analogs. Extending a benzyl group at P-1' to a phenylethyl group in 8 further increases the potency (K-i = 1.4 nM) . Enhanced potency with an extended substituent into the P-3 region wa s observed.