Dioxo-triazines as a novel series of cathepsin K inhibitors

Rankovic, Zoran and Cai, Jiaqiang and Fradera, Xavier and Dempster, Maureen and Mistry, Ashvin and Long, Clive and Hamilton, Emma and King, Angela and Boucharens, Sylviane and Jamieson, Craig and Gillespie, Jonathan and Cumming, Iain and Uitdehaag, Joost and van Zeeland, Mario. (2010) Dioxo-triazines as a novel series of cathepsin K inhibitors. Bioorganic and Medicinal Chemistry Letters, 20 (5). pp. 1488-1490. ISSN 0960-894X

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Abstract

A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory program led to the discovery of potent and selective cathepsin K inhibitors, typified by compd. 24 which displayed IC50 values of 17 nM against catK and >10,000 nM in catL, catB and catS assays.