AMINOPHOSPHONIC ACID-CONTAINING INHIBITORS OF HUMAN COLLAGENASE - MODIFICATION OF THE P-1 RESIDUE

Authors
HUNTER DJ BIRD J CASSIDY F DEMELLO RC HARPER GP KARRAN EH MARKWELL RE MILESWILLIAMS AJ WARD RW
Citation
Dj. Hunter et al., AMINOPHOSPHONIC ACID-CONTAINING INHIBITORS OF HUMAN COLLAGENASE - MODIFICATION OF THE P-1 RESIDUE, Bioorganic & medicinal chemistry letters, 4(24), 1994, pp. 2833-2836
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
24
Year of publication
1994
Pages
2833 - 2836
Database
ISI
SICI code
0960-894X(1994)4:24<2833:AAIOHC>2.0.ZU;2-0
Abstract
A series of peptidomimetic aminophosphonic acid derivatives was synthe sized and evaluated in vitro for inhibition of human fibroblast collag enase activity. Incorporation of a bromonaphthalimidoethyl moiety at t he P-1 position led to potent inhibitors, such as 14a (IC50 0.02 mu M) .