| Literature DB >> 18291644 |
Mark E Salvati1, Aaron Balog, Weifang Shan, Richard Rampulla, Soren Giese, Tom Mitt, Joseph A Furch, Gregory D Vite, Ricardo M Attar, Maria Jure-Kunkel, Jieping Geng, Cheryl A Rizzo, Marco M Gottardis, Stanley R Krystek, Jack Gougoutas, Michael A Galella, Mary Obermeier, Aberra Fura, Gamini Chandrasena.
Abstract
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-(3aalpha,4beta,5beta,7beta,7aalpha)]-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.Entities:
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Year: 2008 PMID： 18291644 DOI： 10.1016/j.bmcl.2008.02.006
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823