Dioxo-triazines as a novel series of cathepsin K inhibitors

A series of potent and selective dioxo-triazine inhibitors of cathepsin K was identified from HTS. A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory programme led to the discovery of potent and selective cathepsin K inhibitors, typified by compound...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1488-1490
Hauptverfasser:	Rankovic, Zoran, Cai, Jiaqiang, Fradera, Xavier, Dempster, Maureen, Mistry, Ashvin, Mitchell, Ann, Long, Clive, Hamilton, Emma, King, Angela, Boucharens, Sylviane, Jamieson, Craig, Gillespie, Jonathan, Cumming, Iain, Uitdehaag, Joost, Zeeland, Mario van
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Catalytic Domain Cathepsin K Cathepsin K - antagonists & inhibitors Cathepsin K - metabolism Crystallography, X-Ray Cysteine protease Cysteine Proteinase Inhibitors - chemical synthesis Cysteine Proteinase Inhibitors - chemistry Cysteine Proteinase Inhibitors - pharmacology High-Throughput Screening Assays Humans Medical sciences Osteoporosis Pharmacology. Drug treatments Structure-Activity Relationship Triazines - chemical synthesis Triazines - chemistry Triazines - pharmacology Uracil - analogs & derivatives Uracil - chemical synthesis Uracil - chemistry Uracil - pharmacology
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Beschreibung
Zusammenfassung:	A series of potent and selective dioxo-triazine inhibitors of cathepsin K was identified from HTS. A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory programme led to the discovery of potent and selective cathepsin K inhibitors, typified by compound 24 which displayed IC 50 values of 17 nM against catK and >10,000 nM in catL, catB and catS assays.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.01.116