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

Research output: Contribution to journalArticle

12 Citations (Scopus)

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

Fingerprint

Cathepsin K
Triazines
Inhibitory Concentration 50
Assays
Cats

Keywords

  • cathepsin L
  • cysteine protease
  • osteoporosis

Cite this

Rankovic, Z., Cai, J., Fradera, X., Dempster, M., Mistry, A., Long, C., ... 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
Rankovic, Zoran ; Cai, Jiaqiang ; Fradera, Xavier ; Dempster, Maureen ; Mistry, Ashvin ; Long, Clive ; Hamilton, Emma ; King, Angela ; Boucharens, Sylviane ; Jamieson, Craig ; Gillespie, Jonathan ; Cumming, Iain ; Uitdehaag, Joost ; van Zeeland, Mario. / Dioxo-triazines as a novel series of cathepsin K inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 5. pp. 1488-1490.
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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, vol. 20, no. 5, pp. 1488-1490. https://doi.org/10.1016/j.bmcl.2010.01.116

Dioxo-triazines as a novel series of cathepsin K inhibitors. / Rankovic, Zoran; Cai, Jiaqiang; Fradera, Xavier; Dempster, Maureen; Mistry, Ashvin; Long, Clive; Hamilton, Emma; King, Angela; Boucharens, Sylviane; Jamieson, Craig; Gillespie, Jonathan; Cumming, Iain; Uitdehaag, Joost; van Zeeland, Mario.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 5, 01.03.2010, p. 1488-1490.

Research output: Contribution to journalArticle

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AU - Rankovic, Zoran

AU - Cai, Jiaqiang

AU - Fradera, Xavier

AU - Dempster, Maureen

AU - Mistry, Ashvin

AU - Long, Clive

AU - Hamilton, Emma

AU - King, Angela

AU - Boucharens, Sylviane

AU - Jamieson, Craig

AU - Gillespie, Jonathan

AU - Cumming, Iain

AU - Uitdehaag, Joost

AU - van Zeeland, Mario.

PY - 2010/3/1

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KW - cysteine protease

KW - osteoporosis

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DO - 10.1016/j.bmcl.2010.01.116

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Rankovic Z, Cai J, Fradera X, Dempster M, Mistry A, Long C et al. Dioxo-triazines as a novel series of cathepsin K inhibitors. Bioorganic and Medicinal Chemistry Letters. 2010 Mar 1;20(5):1488-1490. https://doi.org/10.1016/j.bmcl.2010.01.116