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

…, SM Yang, RH Scannevin, SL Burke, KJ Rhodes…

Index: Zhang, Yue-Mei; Fan, Xiaodong; Yang, Shyh-Ming; Scannevin, Robert H.; Burke, Sharon L.; Rhodes, Kenneth J.; Jackson, Paul F. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 405 - 408

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Citation Number: 30

Abstract

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.