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

doi:10.1016/j.bmcl.2010.01.116

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

Pure And Applied Chemistry

Research output: Contribution to journal › Article › peer-review

25 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 language	English
Pages (from-to)	1488-1490
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2010.01.116
Publication status	Published - 1 Mar 2010

Keywords

cathepsin L
cysteine protease
osteoporosis

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10.1016/j.bmcl.2010.01.116

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title = "Dioxo-triazines as a novel series of cathepsin K inhibitors",

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.",

keywords = "cathepsin L, cysteine protease, osteoporosis",

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

year = "2010",

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doi = "10.1016/j.bmcl.2010.01.116",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Dioxo-triazines as a novel series of cathepsin K inhibitors

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

Y1 - 2010/3/1

N2 - 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.

AB - 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.

KW - cathepsin L

KW - cysteine protease

KW - osteoporosis

UR - https://www.scopus.com/pages/publications/76649126713

U2 - 10.1016/j.bmcl.2010.01.116

DO - 10.1016/j.bmcl.2010.01.116

M3 - Article

SN - 0960-894X

VL - 20

SP - 1488

EP - 1490

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

Dioxo-triazines as a novel series of cathepsin K inhibitors

Abstract

Keywords

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