Literature DB >> 20153187

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

Zoran Rankovic1, Jiaqiang Cai, Xavier Fradera, Maureen Dempster, Ashvin Mistry, Ann Mitchell, Clive Long, Emma Hamilton, Angela King, Sylviane Boucharens, Craig Jamieson, Jonathan Gillespie, Iain Cumming, Joost Uitdehaag, Mario van Zeeland.   

Abstract

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 17nM against catK and >10,000nM in catL, catB and catS assays. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20153187     DOI: 10.1016/j.bmcl.2010.01.116

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Microwave assisted synthesis of some new fused 1,2,4-triazines bearing thiophene moieties with expected pharmacological activity.

Authors:  Hosam A Saad; Mohamed M Youssef; Mosselhi A Mosselhi
Journal:  Molecules       Date:  2011-06-15       Impact factor: 4.411

  1 in total

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