666718-84-9Relevant academic research and scientific papers
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase
Thomas, Sheela A.,Li, Tongmei,Woods, Keith W.,Song, Xiaohong,Packard, Garrick,Fischer, John P.,Diebold, Robert B.,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Johnson, Eric F.,Bouska, Jennifer J.,Olson, Amanda,Guan, Ran,Magnone, Shayna R.,Marsh, Kennan,Luo, Yan,Rosenberg, Saul H.,Giranda, Vincent L.,Li, Qun
, p. 3740 - 3744 (2007/10/03)
Based on lead compounds 2 and 3 a series of 3,5-disubstituted pyridines have been designed and evaluated for inhibition of AKT/PKB. Modifications at the 3 position of the pyridine ring led to a number of potent compounds with improved physical properties, resulting in the identification of 11g as a promising, orally active Akt inhibitor. The synthesis, structure-activity relationship studies, and pharmacokinetic data are presented in this paper.
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
Catalano, John G,Deaton, David N,Furfine, Eric S,Hassell, Annie M,McFadyen, Robert B,Miller, Aaron B,Miller, Larry R,Shewchuk, Lisa M,Willard Jr., Derril H,Wright, Lois L
, p. 275 - 278 (2007/10/03)
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.
