573760-03-9Relevant 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 (2008/12/22)
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.
METHOD FOR THE PREPARATION OF FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF
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, (2008/06/13)
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
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, (2008/06/13)
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
