Dioxo-triazines as a novel series of cathepsin K inhibitors

Zoran Rankovic, Jiaqiang Cai, Xavier Fradera, Maureen Dempster, Ashvin Mistry, Clive Long, Emma Hamilton, Angela King, Sylviane Boucharens, Craig Jamieson, Jonathan Gillespie, Iain Cumming, Joost Uitdehaag, Mario. van Zeeland

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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.
Original languageEnglish
Pages (from-to)1488-1490
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number5
DOIs
Publication statusPublished - 1 Mar 2010

Keywords

  • cathepsin L
  • cysteine protease
  • osteoporosis

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    Rankovic, Z., Cai, J., Fradera, X., Dempster, M., Mistry, A., Long, C., Hamilton, E., King, A., Boucharens, S., Jamieson, C., Gillespie, J., Cumming, I., Uitdehaag, J., & van Zeeland, M. (2010). Dioxo-triazines as a novel series of cathepsin K inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(5), 1488-1490. https://doi.org/10.1016/j.bmcl.2010.01.116