573760-07-3Relevant academic research and scientific papers
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists
Salvati, Mark E.,Balog, Aaron,Shan, Weifang,Rampulla, Richard,Giese, Soren,Mitt, Tom,Furch, Joseph A.,Vite, Gregory D.,Attar, Ricardo M.,Jure-Kunkel, Maria,Geng, Jieping,Rizzo, Cheryl A.,Gottardis, Marco M.,Krystek, Stanley R.,Gougoutas, Jack,Galella, Michael A.,Obermeier, Mary,Fura, Aberra,Chandrasena, Gamini
, p. 1910 - 1915 (2008)
A novel series of [2.2.1]-oxabicyclo imide-based compounds were identified as potent antagonists of the androgen receptor. Molecular modeling and iterative drug design were applied to optimize this series. The lead compound [3aS-(3aα,4β,5β,7β,7aα)]-4-(octahydro-5-hydroxy-4,7-dimethyl-1,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)-2-iodobenzonitrile was shown to have potent in vivo efficacy after oral dosing in the CWR22 human prostate tumor xenograph model.
