Title of article
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists
Author/Authors
Mark E. Salvati، نويسنده , , Aaron Balog، نويسنده , , Weifang Shan، نويسنده , , Richard Rampulla، نويسنده , , Soren Giese، نويسنده , , Tom Mitt، نويسنده , , Joseph A. Furch، نويسنده , , Gregory D. Vite، نويسنده , , Ricardo M. Attar، نويسنده , , Maria Jure-Kunkel، نويسنده , , Jieping Geng، نويسنده , , Cheryl A. Rizzo، نويسنده , , Marco M. Gottardis، نويسنده , , Stanley R. Krystek، نويسنده , , Jack Gougoutas، نويسنده , , Michael A. Galella، نويسنده , , Mary Obermeier، نويسنده , , Aberra Fura، نويسنده , , Gamini Chandrasena، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
1910
To page
1915
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-(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.
Keywords
androgen receptor , AR antagonist , CWR22R , prostate cancer
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799271
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