Literature DB >> 20584610

Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.

Hai-Yun Xiao1, Aaron Balog, Ricardo M Attar, David Fairfax, Linda B Fleming, Christian L Holst, Gregory S Martin, Lana M Rossiter, Jing Chen, Mary-Ellen Cvjic, Janet Dell-John, Jieping Geng, Marco M Gottardis, Wen-Ching Han, Andrew Nation, Mary Obermeier, Cheryl A Rizzo, Liang Schweizer, Thomas Spires, Weifang Shan, Ashvinikumar Gavai, Mark E Salvati, Gregory Vite.   

Abstract

A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20584610     DOI: 10.1016/j.bmcl.2010.06.034

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Diels-Alder reactions of five-membered heterocycles containing one heteroatom.

Authors:  Xiaoyuan Ding; Son T Nguyen; John D Williams; Norton P Peet
Journal:  Tetrahedron Lett       Date:  2014-12-17       Impact factor: 2.415

2.  Mechanism of androgen receptor antagonism by bicalutamide in the treatment of prostate cancer.

Authors:  D J Osguthorpe; A T Hagler
Journal:  Biochemistry       Date:  2011-04-25       Impact factor: 3.162

  2 in total

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