RAPID SYNTHESIS OF NOVEL DIPEPTIDE INHIBITORS OF HUMAN COLLAGENASE AND GELATINASE USING SOLID-PHASE CHEMISTRY

Authors
FOLEY MA HASSMAN AS DREWRY DH GREER DG WAGNER CD FELDMAN PL BERMAN J BICKETT DM MCGEEHAN GM LAMBERT MH GREEN M
Citation
Ma. Foley et al., RAPID SYNTHESIS OF NOVEL DIPEPTIDE INHIBITORS OF HUMAN COLLAGENASE AND GELATINASE USING SOLID-PHASE CHEMISTRY, Bioorganic & medicinal chemistry letters, 6(16), 1996, pp. 1905-1910
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
16
Year of publication
1996
Pages
1905 - 1910
Database
ISI
SICI code
0960-894X(1996)6:16<1905:RSONDI>2.0.ZU;2-N
Abstract
Solid phase chemistry expedited the systematic modification of the C a nd N-terminal groups of cysteine derived lead compound 1 (collagenase IC50 63nM), providing a series of matrix metalloproteinase inhibitors. Potent inhibitors of collagenase (1-2, 4-6, and 10-13) and gelatinase (4-8) were identified. Insights into the binding mode of selective in hibitors will be discussed. Copyright (C) 1996 Elsevier Science Ltd