THE DESIGN, SYNTHESIS, AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF A SERIES OF MACROCYCLIC MMP INHIBITORS

Authors
STEINMAN DH CURTIN ML GARLAND RB DAVIDSEN SK HEYMAN HR HOLMS JH ALBERT DH MAGOC TJ NAGY IB MARCOTTE PA LI JL MORGAN DW HUTCHINS C SUMMERS JB
Citation
Dh. Steinman et al., THE DESIGN, SYNTHESIS, AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF A SERIES OF MACROCYCLIC MMP INHIBITORS, Bioorganic & medicinal chemistry letters, 8(16), 1998, pp. 2087-2092
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
16
Year of publication
1998
Pages
2087 - 2092
Database
ISI
SICI code
0960-894X(1998)8:16<2087:TDSASO>2.0.ZU;2-7
Abstract
A series of succinate-derived hydroxamic acids incorporating a macrocy clic ring were designed, synthesized, and evaluated as inhibitors of m atrix metalloproteinases. The inhibitors were designed based on the pu blished X-ray crystal structure of batimastat (1) complexed with human neutrophil collagenase (MMP-8). The synthesized compounds were shown to inhibit selected MMPs in vitro with low nanomolar potency. (C) 1998 Elsevier Science Ltd. All rights reserved.