Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors

descriptionPublicationkeyboard_double_arrow_right Article 01 Aug 2007 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 17, pages 4,333-4,337 (issn: 0960-894X,

Authors: Henry-Georges, Lombart; Eric, Feyfant; Diane, Joseph-McCarthy; Adrian, Huang; Frank, Lovering; LinHong, Sun; Yi, Zhu; +3 Authors

doi: 10.1016/j.bmcl.2007.05.022

pmid: 17531482

Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors

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Abstract

Structure-based methods were used to design beta-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13. Several compounds in this series were synthesized and evaluated in enzymatic and cell-based assays. These analogs exhibit excellent in vitro potency against isolated TACE enzyme and show good selectivity for TACE over the related metalloproteases MMP-2, -13, and -14.

Keywords

Models, Molecular, ADAM Proteins, Drug Design, ADAM17 Protein, Enzyme Inhibitors, Hydroxamic Acids

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BindingDB Entry 50020447: Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.
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Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors

Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors

1 Research products, page 1 of 1

BindingDB Entry 50020447: Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.