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Review | Special issue | Vol 70, No. 1, 2006, pp.691-704
Published online, 17th November, 2006
DOI: 10.3987/REV-06-SR(W)2
Heterocyclic Inhibitors of Tumor Necrosis Factor-α Converting Enzyme (TACE)

Jeremy I. Levin

*Chemical and Screening Sciences, Wyeth Inc., 401 N. Middletown Rd., Pearl River, NY 10965, U.S.A.


A variety of heterocyclic ring systems have been prepared as scaffolds for butynyloxyphenyl sulfonamide and sulfone hydroxamic acid inhibitors of TACE enzyme. All scaffolds provided highly active TACE inhibitors, but selectivity, and cellular activity was highly scaffold dependent.