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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. doi: 10.1016/j.bmcl.2010.01.100. Epub 2010 Jan 25.

Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.

Author information

1
Schering-Plough Corporation, Newhouse, Lanarkshire, ML1 5SH Scotland, United Kingdom. zoran.rankovic@spcorp.com

Abstract

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 (IC(50)=4nM), >580-fold selectivity over catL and catB, and oral bioavailability in the rat of 52%.

PMID:
20149657
DOI:
10.1016/j.bmcl.2010.01.100
[Indexed for MEDLINE]

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