1403587-95-0Relevant academic research and scientific papers
Highly selective azadipeptide nitrile inhibitors for cathepsin K: Design, synthesis and activity assays
Ren, Xing-Feng,Li, Hong-Wei,Fang, Xuexun,Wu, Yuqing,Wang, Lincong,Zou, Shuxue
, p. 1143 - 1148 (2013/03/28)
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 (Ki = 0.0031 nM), but also highly selective over both cathepsins B and S (～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.
