| Literature DB >> 21300546 |
Chris De Savi1, Andrew Pape, John G Cumming, Attilla Ting, Peter D Smith, Jeremy N Burrows, Mark Mills, Chris Davies, Scott Lamont, David Milne, Calum Cook, Peter Moore, Yvonne Sawyer, Stefan Gerhardt.
Abstract
Two series of N-hydroxyformamide inhibitors of ADAM-TS4 were identified from screening compounds previously synthesised as inhibitors of matrix metalloproteinase-13 (collagenase-3). Understanding of the binding mode of this class of compound using ADAM-TS1 as a structural surrogate has led to the discovery of potent and very selective inhibitors with favourable DMPK properties. Synthesis, structure-activity relationships, and strategies to improve selectivity and lower in vivo metabolic clearance are described.Entities:
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Year: 2011 PMID： 21300546 DOI： 10.1016/j.bmcl.2011.01.036
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823