1219941-44-2Relevant academic research and scientific papers
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors
Cai, Jiaqiang,Bennett, D. Jonathan,Rankovic, Zoran,Dempster, Maureen,Fradera, Xavier,Gillespie, Jonathan,Cumming, Iain,Finlay, William,Baugh, Mark,Boucharens, Sylviane,Bruin, John,Cameron, Kenneth S.,Hamilton, William,Kerr, Jennifer,Kinghorn, Emma,McGarry, George,Robinson, John,Scullion, Paul,Uitdehaag, Joost C.M.,Van Zeeland, Mario,Potin, Dominique,Saniere, Laurent,Fouquet, Andre,Chevallier, Francois,Deronzier, Hortense,Dorleans, Cecile,Nicolai, Eric
scheme or table, p. 4447 - 4450 (2010/10/02)
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.
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors
Rankovic, Zoran,Cai, Jiaqiang,Kerr, Jennifer,Fradera, Xavier,Robinson, John,Mistry, Ashvin,Hamilton, Emma,McGarry, George,Andrews, Fiona,Caulfield, Wilson,Cumming, Iain,Dempster, Maureen,Waller, John,Scullion, Paul,Martin, Iain,Mitchell, Ann,Long, Clive,Baugh, Mark,Westwood, Paul,Kinghorn, Emma,Bruin, John,Hamilton, William,Uitdehaag, Joost,Zeeland, Mario van,Potin, Dominique,Saniere, Laurent,Fouquet, Andre,Chevallier, Fran?ois,Deronzier, Hortense,Dorleans, Cecile,Nicolai, Eric
scheme or table, p. 1524 - 1527 (2010/06/21)
Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with good pharmacokinetic profiles, for example, compound 20 showed high catK potency (IC50 = 4 nM), >580-fold selectivity over catL and catB, and oral bioavailability in the rat of 52%.
