1. 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
- Author
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Cai J, Bennett DJ, Rankovic Z, Dempster M, Fradera X, Gillespie J, Cumming I, Finlay W, Baugh M, Boucharens S, Bruin J, Cameron KS, Hamilton W, Kerr J, Kinghorn E, McGarry G, Robinson J, Scullion P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, and Nicolai E
- Subjects
- Catalytic Domain, Cathepsin K antagonists & inhibitors, Cathepsin K metabolism, Cathepsins metabolism, Cell Line, Computer Simulation, Humans, Nitriles chemical synthesis, Nitriles pharmacology, Protease Inhibitors chemical synthesis, Protease Inhibitors pharmacology, Purines chemical synthesis, Purines pharmacology, Pyrimidines chemistry, Cathepsins antagonists & inhibitors, Nitriles chemistry, Protease Inhibitors chemistry, Purines chemistry
- Abstract
Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl)pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide potent and selective cathepsin S inhibitors., (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Published
- 2010
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