Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs)

Several classes of arylsulfone-based MMP-2/-9 inhibitors utilizing 6-to 8-membered heterocyclic rings as zinc-binding groups (ZBGs) have been synthesized and their enzyme inhibitory activities were evaluated. The most potent arylsulfone inhibitors are based on the rigid 1- or 3-hydroxypyridone ZBG....

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008, Vol.18 (1), p.405-408
Hauptverfasser:	Zhang, Yue-Mei, Fan, Xiaodong, Yang, Shyh-Ming, Scannevin, Robert H., Burke, Sharon L., Rhodes, Kenneth J., Jackson, Paul F.
Format:	Artikel
Sprache:	eng
Schlagworte:	Arylsulfone Biological and medical sciences Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology Lactams - chemical synthesis Lactams - chemistry Lactams - pharmacology Matrix metalloproteinase inhibitor Matrix Metalloproteinase Inhibitors Medical sciences Miscellaneous MMP-2 MMP-9 Pharmacology. Drug treatments Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Pyridones - chemistry Pyridones - pharmacology Structure-Activity Relationship Sulfones - chemical synthesis Sulfones - chemistry Sulfones - pharmacology Zinc - chemistry Zinc-binding group
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Several classes of arylsulfone-based MMP-2/-9 inhibitors utilizing 6-to 8-membered heterocyclic rings as zinc-binding groups (ZBGs) have been synthesized and their enzyme inhibitory activities were evaluated. The most potent arylsulfone inhibitors are based on the rigid 1- or 3-hydroxypyridone ZBG. Several classes of arylsulfone-based MMP-2/-9 inhibitors utilizing 6- to 8-membered heterocyclic rings as zinc-binding groups (ZBGs) have been synthesized and their enzyme inhibitory activities were evaluated. Although a number of 6- and 7-membered heterocycles were effective, the most potent arylsulfone inhibitors are based on the rigid 1- or 3-hydroxypyridone ZBG.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.10.049