☆ 4.6 Article

Highly selective azadipeptide nitrile inhibitors for cathepsin K: design, synthesis and activity assays

ORGANIC & BIOMOLECULAR CHEMISTRY (2013)

期刊

ORGANIC & BIOMOLECULAR CHEMISTRY

卷 11, 期 7, 页码 1143-1148

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ROYAL SOC CHEMISTRY

DOI: 10.1039/c2ob26624e

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Chemistry, Organic

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NSFC [20973073, 20934002, 91027027]
State Key Laboratory of Supramolecular Structure and Materials, Jilin University

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We have developed a series of azadipeptide nitriles with different P3 groups. A triaryl meta-phenyl derivative, compound 13, was not only a potent inhibitor for cathepsin K (K-i = 0.0031 nM), but also highly selective over both cathepsins B and S (similar to 1000-fold). A protein-ligand docking study performed on the series provided a possible explanation why compound 13 could be significantly more potent than the others, especially compound 12 in the same series.

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